Pub Date : 2022-06-20DOI: 10.2174/2210303112666220620093106
S. Bhattacharyya, A. Verma
Memory disorders require a steady-state balance of choline and cytidine. Citicoline is prescribed as an exogenous source of choline and cytidine. The present study proposes a mucoadhesive multiparticulate sustained delivery of citicoline as a supportive control for memory loss. The formulation of citicoline sodium microparticles was done by ionotropic gelation method using alginate and hydroxypropyl methylcellulose (HPMC) in three different ratios. The three formulations were preliminary evaluated for the in vitro drug release study. Depending on their release pattern, a simplex lattice mixture design of 21 trial runs, with a set of possible combinations of each component of the three formulations was employed to get an optimized ratio that could attend a predetermined release of drug at 1st, 4th, 6th, and 8th h. The optimized product was characterized for physicochemical evaluation, thermal analysis, in vitro drug release, surface morphology, and stability study. Optimization of the design yielded a ratio that could prolong the release as predicted by the design. The release mechanism followed non-Fickian diffusion. Differential thermal analysis exhibited high drug entrapment in the microparticles. Surface morphology studies revealed that drug release took place by the formation of channels. Stability studies indicated there was no change in the properties even after six months and the moisture retention was meagre. The employed simplex lattice design could be successfully used to make microparticles of predetermined release characteristics with a steady-state release of the drug and can be a promising approach to provide an affordable therapy of citicoline to improve its effectivity.
{"title":"Preparation and characterization of multicomponent particles for controlled and tunable release of citicoline","authors":"S. Bhattacharyya, A. Verma","doi":"10.2174/2210303112666220620093106","DOIUrl":"https://doi.org/10.2174/2210303112666220620093106","url":null,"abstract":"\u0000\u0000Memory disorders require a steady-state balance of choline and cytidine. Citicoline is prescribed as an exogenous source of choline and cytidine.\u0000\u0000\u0000\u0000The present study proposes a mucoadhesive multiparticulate sustained delivery of citicoline as a supportive control for memory loss.\u0000\u0000\u0000\u0000The formulation of citicoline sodium microparticles was done by ionotropic gelation method using alginate and hydroxypropyl methylcellulose (HPMC) in three different ratios. The three formulations were preliminary evaluated for the in vitro drug release study. Depending on their release pattern, a simplex lattice mixture design of 21 trial runs, with a set of possible combinations of each component of the three formulations was employed to get an optimized ratio that could attend a predetermined release of drug at 1st, 4th, 6th, and 8th h. The optimized product was characterized for physicochemical evaluation, thermal analysis, in vitro drug release, surface morphology, and stability study.\u0000\u0000\u0000\u0000Optimization of the design yielded a ratio that could prolong the release as predicted by the design. The release mechanism followed non-Fickian diffusion. Differential thermal analysis exhibited high drug entrapment in the microparticles. Surface morphology studies revealed that drug release took place by the formation of channels. Stability studies indicated there was no change in the properties even after six months and the moisture retention was meagre.\u0000\u0000\u0000\u0000The employed simplex lattice design could be successfully used to make microparticles of predetermined release characteristics with a steady-state release of the drug and can be a promising approach to provide an affordable therapy of citicoline to improve its effectivity.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44645883","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Periodontitis is a serious gum infection associated with inflammation of the periodontium around the teeth. Based on the etiology and pathogenesis, periodontitis has several conventional treatment strategies. Treatment with antibiotics and antimicrobials is the most common therapy. However, development of drug resistance and the manifestation of side effects make conventional strategies ineffective. In the last decades, local drug delivery in the periodontal pocket has gained significant attention as a novel strategy. Sustained release of drug at the target site (periodontal pocket) for a prolonged period is the main advantage over conventional therapy. Bioadhesive periodontal films are mostly used. They are thin films made up of unique mixtures of bioadhesive polymers, binders, plasticizers, and drug release modifiers. They can be loaded with antibiotics, metal nanoparticles, metal oxide nanoparticles, or a combination of them. The dried film is cut into a suitable size and inserted into the periodontal pocket for direct delivery of therapeutic agents. Thus, a smaller dose is required and systemic side effects are avoided. In this manuscript, the pathophysiology of periodontitis, the role of biofilm formation, development of periodontal film loaded with antibiotics and nanoparticles have been reviewed and the future aspects have been discussed.
{"title":"Periodontal Film: A Potential Treatment Strategy Of Periodontitis","authors":"Debabrata Ghosh Dastidar, Avinandan Ash, D. Saha, Poulomi Chakraborty, Prosun Tribedi","doi":"10.2174/2210303112666220617110030","DOIUrl":"https://doi.org/10.2174/2210303112666220617110030","url":null,"abstract":"\u0000\u0000Periodontitis is a serious gum infection associated with inflammation of the periodontium around the teeth. Based on the etiology and pathogenesis, periodontitis has several conventional treatment strategies. Treatment with antibiotics and antimicrobials is the most common therapy. However, development of drug resistance and the manifestation of side effects make conventional strategies ineffective. In the last decades, local drug delivery in the periodontal pocket has gained significant attention as a novel strategy. Sustained release of drug at the target site (periodontal pocket) for a prolonged period is the main advantage over conventional therapy. Bioadhesive periodontal films are mostly used. They are thin films made up of unique mixtures of bioadhesive polymers, binders, plasticizers, and drug release modifiers. They can be loaded with antibiotics, metal nanoparticles, metal oxide nanoparticles, or a combination of them. The dried film is cut into a suitable size and inserted into the periodontal pocket for direct delivery of therapeutic agents. Thus, a smaller dose is required and systemic side effects are avoided. In this manuscript, the pathophysiology of periodontitis, the role of biofilm formation, development of periodontal film loaded with antibiotics and nanoparticles have been reviewed and the future aspects have been discussed.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43145116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-06-02DOI: 10.2174/2210303112666220602123548
R. Rani, Manish Kumar, R. Verma, Pravin Gupta, B. Kumari, R. Pahwa, Vineet Mittal, S. Bhatt, Deepak Kaushik
Microspheres are controlled drug delivery systems (CDDS) because they have the potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include biocompatiblity, greater bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects which restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to absorb the drug in the stomach for better antiulcer potential and fewer side effects. The rationale of the current investigational effort is to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interaction with the mucosa inside the stomach. The capillary extrusion technique was used with the aid of chitosan, a polymer in addition to sodium lauryl sulphate, a crosslinking agent. Scanning electron microscopy characterized the surface morphology of the prepared microspheres. The effects of polymeric concentration as well as the concentration of cross-link agent on percent yield, in vitro floating behavior, and in vitro drug release were efficiently assessed. Diffusion has been observed as a popular mechanism for most launches. Prolonged drug release (12 hrs) has been seen in the prepared microspheres and they also remained buoyant for around 10 hrs. In vivo evaluation study was successfully performed. From the values of ulcer indexes for various groups, percentage protection was determined. The treatment group (F-2 formulation) showed the maximum percentage protection of 97.29%. The prepared floating microspheres can thus persuade potential candidates to be adaptable to any intra-gastric conditions for multiple-unit delivery devices.
{"title":"Berberine hydrochloride embedded chitosan-based novel floating microspheres: Optimization, characterization and in vivo anti-ulcer potential","authors":"R. Rani, Manish Kumar, R. Verma, Pravin Gupta, B. Kumari, R. Pahwa, Vineet Mittal, S. Bhatt, Deepak Kaushik","doi":"10.2174/2210303112666220602123548","DOIUrl":"https://doi.org/10.2174/2210303112666220602123548","url":null,"abstract":"\u0000\u0000Microspheres are controlled drug delivery systems (CDDS) because they have the potential to encapsulate various drugs, nucleic acids, and proteins. Their benefits include biocompatiblity, greater bioavailability, and controlled release. Presently, existing antiulcer agents suffer from severe side effects which restricted their utility and encouraged the requirement of a harmless and proficient new antiulcer agent. The rationale of the present research work was to absorb the drug in the stomach for better antiulcer potential and fewer side effects.\u0000\u0000\u0000\u0000The rationale of the current investigational effort is to prepare and examine floating microspheres using berberine hydrochloride to increase gastric retention without interaction with the mucosa inside the stomach.\u0000\u0000\u0000\u0000The capillary extrusion technique was used with the aid of chitosan, a polymer in addition to sodium lauryl sulphate, a crosslinking agent. Scanning electron microscopy characterized the surface morphology of the prepared microspheres. The effects of polymeric concentration as well as the concentration of cross-link agent on percent yield, in vitro floating behavior, and in vitro drug release were efficiently assessed.\u0000\u0000\u0000\u0000Diffusion has been observed as a popular mechanism for most launches. Prolonged drug release (12 hrs) has been seen in the prepared microspheres and they also remained buoyant for around 10 hrs. In vivo evaluation study was successfully performed. From the values of ulcer indexes for various groups, percentage protection was determined. The treatment group (F-2 formulation) showed the maximum percentage protection of 97.29%.\u0000\u0000\u0000\u0000The prepared floating microspheres can thus persuade potential candidates to be adaptable to any intra-gastric conditions for multiple-unit delivery devices.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42566599","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-18DOI: 10.2174/2210303112666220518164608
Nikhil Sutar, P. Karwa
Amitriptyline hydrochloride is a Tricyclic Antidepressant (TCA) belonging to BCS class I exhibiting only 30-60% bioavailability and often coupled with poor patient compliance. The primary objective was to develop a formulation with commercial viability and to reduce dosing frequency in order to promote adherence of depressed patients to the treatment regime. The study also focused on reducing the dose of amitriptyline by controlling the release using osmotic technology; thereby reducing the side effects of amitriptyline. Controlled Porosity Osmotic Pump (CPOP) systems eliminate the need for expensive drilling processes and in turn are apt for industrial manufacturing systems where as other osmotic systems have practical limitations. Wet granulation technique was used for the formulation of CPOP tablets of amitriptyline as burst release was observed in directly compressed tablets. Screening of polymers, osmogen and weight gain were performed. F6-D3 (3 % Di-butyl phthalate) with lactose as osmogen and HPMC K 35 M as polymer was optimized. The drug release from the optimized formulation was found to be independent of the effect of agitational intensity and pH. To confirm the osmotic release mechanism, the osmotic pressure of the dissolution medium was increased. The drug release decreased markedly due to an increase in osmotic pressure. Accelerated Stability studies were carried out in ICH certified stability chambers as per the specifications and were found to be stable. It was evident that osmotic pressure generated within the CPOP tablets along with the controlled formation of pores using Cellulose Acetate (CA-398-10 EP/ NP) was able to control the release of amitriptyline hydrochloride for 24 hours. Thus, the Oral Osmotic Drug Delivery system is a promising technology for product life-cycle strategies.
{"title":"Effect Of Cellulose Acetate (Ca-398-10 Ep/ Np) On\u0000Osmotically Controlled Drug Delivery System Of Amitriptyline","authors":"Nikhil Sutar, P. Karwa","doi":"10.2174/2210303112666220518164608","DOIUrl":"https://doi.org/10.2174/2210303112666220518164608","url":null,"abstract":"\u0000\u0000Amitriptyline hydrochloride is a Tricyclic Antidepressant (TCA) belonging to BCS class I exhibiting only 30-60% bioavailability and often coupled with poor patient compliance. The primary objective was to develop a formulation with commercial viability and to reduce dosing frequency in order to promote adherence of depressed patients to the treatment regime. The study also focused on reducing the dose of amitriptyline by controlling the release using osmotic technology; thereby reducing the side effects of amitriptyline.\u0000\u0000\u0000\u0000Controlled Porosity Osmotic Pump (CPOP) systems eliminate the need for expensive drilling processes and in turn are apt for industrial manufacturing systems where as other osmotic systems have practical limitations. Wet granulation technique was used for the formulation of CPOP tablets of amitriptyline as burst release was observed in directly compressed tablets. Screening of polymers, osmogen and weight gain were performed.\u0000\u0000\u0000\u0000F6-D3 (3 % Di-butyl phthalate) with lactose as osmogen and HPMC K 35 M as polymer was optimized. The drug release from the optimized formulation was found to be independent of the effect of agitational intensity and pH. To confirm the osmotic release mechanism, the osmotic pressure of the dissolution medium was increased. The drug release decreased markedly due to an increase in osmotic pressure.\u0000\u0000\u0000\u0000Accelerated Stability studies were carried out in ICH certified stability chambers as per the specifications and were found to be stable. It was evident that osmotic pressure generated within the CPOP tablets along with the controlled formation of pores using Cellulose Acetate (CA-398-10 EP/ NP) was able to control the release of amitriptyline hydrochloride for 24 hours. Thus, the Oral Osmotic Drug Delivery system is a promising technology for product life-cycle strategies.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48682168","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-12DOI: 10.2174/2210303112666220512154520
K. Pathak, R. Das, Riya Saikia, J. Sahariah, Hemanta Pathak, H. Sarma, Aparoop Das
Gallic acid is a natural phenolic compound found in several fruits and medicinal plants. It is reported to have several health-promoting effects including antioxidant, anti-inflammatory, diabetic, antineoplastic properties, gastrointestinal, neuropsychological, metabolic and cardiovascular disorders. The aim of the present work was to study the influence of formulation factors on the physicochemical properties of gallic acid-loaded chitosan nanoparticles in order to optimize the formulation. Active chitosan nanoparticles could be used to support the modification of gallic acid delivery. The nanoparticles were prepared by the emulsification solvent evaporation method using sonication. A 3-factor, 2-level BBD (Box-Behnken Design) was applied for exploring and optimizing the main effects, quadratic effects as well as interaction effects of the ingredients of the formulation on the performance of the nanoparticles. The responses like particle size, polydispersity index, zeta potential and encapsulation efficiency were also determined. The concentration of gallic acid nanoparticles seems to be the most critical element affecting their properties. The concentration of chitosan was increased, which resulted in an increase in particle size. The optimised drug-loaded nanoparticles have a zeta potential of -5.2 mV due to their largely negative surface charge. Although the measured zeta potential was low, the nanoparticle dispersion remained stable, and no significant change in the shape or particle size of the gallic acid-loaded chitosan nanoparticles was seen after two weeks at 4°C. The gallic acid-loaded nanoparticles have a particle size of 230 nm. Gallic acid reduced the particle size after it was added. One probable explanation for this is that the loaded medicine increased the cohesive force of the hydrophobic contact, resulting in the size reduction. A formulation was optimised based on the acquired results, and the experimental values were comparable to the expected values. FTIR examination revealed that gallic acid-loaded chitosan nanoparticles displayed both hydrogen bond and ionic interactions, allowing for active agent encapsulation and augmentation. The overall results indicated that decreasing the chitosan concentration drug entrapement efficiency increases and gallic acid concentration was the main factor influencing particle size, while entrapment efficiency was predominantly affected by the chitosan concentration.
{"title":"Design and fabrication of gallic acid loaded chitosan nanoformulation","authors":"K. Pathak, R. Das, Riya Saikia, J. Sahariah, Hemanta Pathak, H. Sarma, Aparoop Das","doi":"10.2174/2210303112666220512154520","DOIUrl":"https://doi.org/10.2174/2210303112666220512154520","url":null,"abstract":"\u0000\u0000Gallic acid is a natural phenolic compound found in several fruits and medicinal plants. It is reported to have several health-promoting effects including antioxidant, anti-inflammatory, diabetic, antineoplastic properties, gastrointestinal, neuropsychological, metabolic and cardiovascular disorders.\u0000\u0000\u0000\u0000The aim of the present work was to study the influence of formulation factors on the physicochemical properties of gallic acid-loaded chitosan nanoparticles in order to optimize the formulation.\u0000\u0000\u0000\u0000Active chitosan nanoparticles could be used to support the modification of gallic acid delivery. The nanoparticles were prepared by the emulsification solvent evaporation method using sonication. A 3-factor, 2-level BBD (Box-Behnken Design) was applied for exploring and optimizing the main effects, quadratic effects as well as interaction effects of the ingredients of the formulation on the performance of the nanoparticles. The responses like particle size, polydispersity index, zeta potential and encapsulation efficiency were also determined.\u0000\u0000\u0000\u0000The concentration of gallic acid nanoparticles seems to be the most critical element affecting their properties. The concentration of chitosan was increased, which resulted in an increase in particle size. The optimised drug-loaded nanoparticles have a zeta potential of -5.2 mV due to their largely negative surface charge. Although the measured zeta potential was low, the nanoparticle dispersion remained stable, and no significant change in the shape or particle size of the gallic acid-loaded chitosan nanoparticles was seen after two weeks at 4°C. The gallic acid-loaded nanoparticles have a particle size of 230 nm. Gallic acid reduced the particle size after it was added. One probable explanation for this is that the loaded medicine increased the cohesive force of the hydrophobic contact, resulting in the size reduction. A formulation was optimised based on the acquired results, and the experimental values were comparable to the expected values. FTIR examination revealed that gallic acid-loaded chitosan nanoparticles displayed both hydrogen bond and ionic interactions, allowing for active agent encapsulation and augmentation.\u0000\u0000\u0000\u0000The overall results indicated that decreasing the chitosan concentration drug entrapement efficiency increases and gallic acid concentration was the main factor influencing particle size, while entrapment efficiency was predominantly affected by the chitosan concentration.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48923938","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-04-28DOI: 10.2174/2210303112666220428101738
Km. Reena, L. Singh
Psoriasis is a long-term chronic inflammatory, autoimmune and reoccurring skin condition. About 2% to 5% of the world's population is impacted by psoriasis. People affected by psoriasis are more prone to develop other health conditions including psoriatic arthritis, anxiety, depression and cardiovascular disorders. Long-term use of several synthetic medications used for their management have been showing typical severe side effects. Curcumin, a natural compound generated from the golden spice (Curcuma longa) has been recommended as a potential alternative for the management of psoriasis. Curcumin works at molecular level by binding with the various inflammatory receptors that play key role in the initiation of psoriasis. The aim of this review is to report the use and discuss the mechanism of action of curcumin in the management of psoriasis, and mutually to overcome the side effects shown by the synthetic medications. Qualitative literature review Pub Med, Scopus, Web of Science, Google Scholar, Google Books, Science Direct meet the inclusion criteria. As a traditional herb curcumin appears as a beneficiary medicament because of its anti-oxidant, anti-inflammatory and immune-modulating activities proposing minimal side effects. Thereby ensuring its defensive mechanism towards psoriasis.
牛皮癣是一种长期慢性炎症，自身免疫性和反复发生的皮肤状况。世界上约2%至5%的人口受到牛皮癣的影响。受牛皮癣影响的人更容易出现其他健康问题，包括银屑病关节炎、焦虑、抑郁和心血管疾病。长期使用几种用于治疗的合成药物已显示出典型的严重副作用。姜黄素是一种由黄金香料(姜黄)产生的天然化合物，已被推荐为治疗牛皮癣的潜在替代品。姜黄素在分子水平上通过与各种炎症受体结合起作用，这些炎症受体在牛皮癣的发病中起关键作用。本文就姜黄素在银屑病治疗中的应用及作用机制进行综述，并探讨其在银屑病治疗中的作用机制。质性文献综述Pub Med、Scopus、Web of Science、谷歌Scholar、谷歌Books、Science Direct符合纳入标准。作为一种传统的草药，姜黄素因其抗氧化、抗炎和免疫调节活性而成为一种有益的药物，副作用最小。从而确保其对牛皮癣的防御机制。
{"title":"Curcumin: A review of its’ efficacy in the management of psoriasis","authors":"Km. Reena, L. Singh","doi":"10.2174/2210303112666220428101738","DOIUrl":"https://doi.org/10.2174/2210303112666220428101738","url":null,"abstract":"\u0000\u0000Psoriasis is a long-term chronic inflammatory, autoimmune and reoccurring skin condition. About 2% to 5% of the world's population is impacted by psoriasis. People affected by psoriasis are more prone to develop other health conditions including psoriatic arthritis, anxiety, depression and cardiovascular disorders. Long-term use of several synthetic medications used for their management have been showing typical severe side effects. Curcumin, a natural compound generated from the golden spice (Curcuma longa) has been recommended as a potential alternative for the management of psoriasis. Curcumin works at molecular level by binding with the various inflammatory receptors that play key role in the initiation of psoriasis.\u0000\u0000\u0000\u0000The aim of this review is to report the use and discuss the mechanism of action of curcumin in the management of psoriasis, and mutually to overcome the side effects shown by the synthetic medications.\u0000\u0000\u0000\u0000Qualitative literature review Pub Med, Scopus, Web of Science, Google Scholar, Google Books, Science Direct meet the inclusion criteria.\u0000\u0000\u0000\u0000As a traditional herb curcumin appears as a beneficiary medicament because of its anti-oxidant, anti-inflammatory and immune-modulating activities proposing minimal side effects. Thereby ensuring its defensive mechanism towards psoriasis.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42992870","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-04-14DOI: 10.2174/2210303112666220414100934
Nisha K. Singh, S. Dey, B. Kumar, P. Sahoo
Osteoporosis is a chronic, progressive bone condition which is mostly prevalent in post-menopausal women and the elderly population. An imbalance in the natural bone remodeling process which is involved in the formation of bone and resorption is responsible for osteoporosis leading to bone fragility. It shows no clinical manifestation until a fracture takes place. Osteoporosis is a global epidemic which reduces quality of life, increases the chances of disabilities and adds on a huge financial load. Early diagnosis and treatment can help in preventing the disease. Several drug regimens are used in treating the condition however the drugs are accompanied by several adverse effects. Nutraceuticals like herbs, minerals, vitamins, dairy products and minerals support skeletal strength and integrity. Therefore, use of different types of nutraceuticals can improve overall bone strength and provide improved treatment of osteoporosis. The review paper focusses on providing in depth knowledge about the various nutraceuticals that are used in the management of osteoporosis along with the novel nanotechnology based delivery approaches for enhanced delivery of nutraceuticals as the advent of nanotechnology in pharmaceuticals have opened new avenues in the challenging arena of nutraceuticals for providing benefits like stability, higher efficiency, solubility, enhanced bioavailability, permeability and production without additives.
{"title":"A comprehensive review on nanotechnological approaches for enhanced delivery of nutraceuticals in the management of osteoporosis","authors":"Nisha K. Singh, S. Dey, B. Kumar, P. Sahoo","doi":"10.2174/2210303112666220414100934","DOIUrl":"https://doi.org/10.2174/2210303112666220414100934","url":null,"abstract":"\u0000\u0000Osteoporosis is a chronic, progressive bone condition which is mostly prevalent in post-menopausal women and the elderly population. An imbalance in the natural bone remodeling process which is involved in the formation of bone and resorption is responsible for osteoporosis leading to bone fragility. It shows no clinical manifestation until a fracture takes place. Osteoporosis is a global epidemic which reduces quality of life, increases the chances of disabilities and adds on a huge financial load. Early diagnosis and treatment can help in preventing the disease. Several drug regimens are used in treating the condition however the drugs are accompanied by several adverse effects. Nutraceuticals like herbs, minerals, vitamins, dairy products and minerals support skeletal strength and integrity. Therefore, use of different types of nutraceuticals can improve overall bone strength and provide improved treatment of osteoporosis. The review paper focusses on providing in depth knowledge about the various nutraceuticals that are used in the management of osteoporosis along with the novel nanotechnology based delivery approaches for enhanced delivery of nutraceuticals as the advent of nanotechnology in pharmaceuticals have opened new avenues in the challenging arena of nutraceuticals for providing benefits like stability, higher efficiency, solubility, enhanced bioavailability, permeability and production without additives.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46936914","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-04-13DOI: 10.2174/2210303112666220413081911
Yi Ying Loh, A. A. Enose, Vandana Garg
Tablet coating has evolved over the years and today, there are various types of coating for delayed release of a drug. Drugs can be enteric-coated to provide delayed release, protect the active pharmaceutical ingredients, minimize undesirable effects, and modify the pharmacokinetic properties of a drug, which will have clinical impacts. There are certain types of drugs that need to be enteric coated due to various reasons, such as it being a gastric irritant or it being acid liable. This article will review ethylcellulose and polymethacrylate, their role in an enteric coating, and their process coating parameters. Ethylcellulose can be used to provide a short delayed release; it can be modified by adding pH-dependent polymers such as sodium alginate and hydroxypropyl methylcellulose phthalate for a long delayed release. On the other hand, polymethacrylate can also be employed to enteric coat drugs without additional polymers. Polymethacrylate such as Eudragit comes in different grades with varying proportions of polymer ratio, allowing for targeted delayed drug release. These will impact which polymer to be employed. Upon choosing the coating material of choice, modeling can also be employed to predict in vitro and in vivo correlation as enteric-coated products can have unpredictable in vivo PK profiles. Today, the trend is moving away from the traditional coating and towards new polymers, and with digitalization, there is a focus to start using data from laboratory experiments to be integrated with computational modeling, artificial intelligence, and machine learning to accurately predict key process parameters and film properties for high-quality products.
{"title":"Enteric Coating Polymers Past and Present - A review","authors":"Yi Ying Loh, A. A. Enose, Vandana Garg","doi":"10.2174/2210303112666220413081911","DOIUrl":"https://doi.org/10.2174/2210303112666220413081911","url":null,"abstract":"\u0000\u0000Tablet coating has evolved over the years and today, there are various types of coating for delayed release of a drug. Drugs can be enteric-coated to provide delayed release, protect the active pharmaceutical ingredients, minimize undesirable effects, and modify the pharmacokinetic properties of a drug, which will have clinical impacts. There are certain types of drugs that need to be enteric coated due to various reasons, such as it being a gastric irritant or it being acid liable. This article will review ethylcellulose and polymethacrylate, their role in an enteric coating, and their process coating parameters. Ethylcellulose can be used to provide a short delayed release; it can be modified by adding pH-dependent polymers such as sodium alginate and hydroxypropyl methylcellulose phthalate for a long delayed release. On the other hand, polymethacrylate can also be employed to enteric coat drugs without additional polymers. Polymethacrylate such as Eudragit comes in different grades with varying proportions of polymer ratio, allowing for targeted delayed drug release. These will impact which polymer to be employed. Upon choosing the coating material of choice, modeling can also be employed to predict in vitro and in vivo correlation as enteric-coated products can have unpredictable in vivo PK profiles. Today, the trend is moving away from the traditional coating and towards new polymers, and with digitalization, there is a focus to start using data from laboratory experiments to be integrated with computational modeling, artificial intelligence, and machine learning to accurately predict key process parameters and film properties for high-quality products.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44253959","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-04-12DOI: 10.2174/2210303112666220412134241
Mohit Kumar Tomar, S. Pahwa, L. Tyagi, C. Gupta, Preeti Maan, V. Sethi
Microsponge drug delivery systems comprise of spherical and porous microspheres used for prolonged topical drug delivery. These systems considerably reduce the undesirable side effects, offering improved patient compliance and reduced dosing frequency. The present study was focused on the development of topical controlled release preparations of microsponges loaded gel of clarithromycin with the purpose to cure bacterial skin infections. Four batches of Microsponges (F1, F2, F3, and F4) of clarithromycin (CLR) containing fixed amounts of clarithromycin (100 mg), Dichloromethane (5 ml), polyvinyl alcohol (5 % w/v) and distilled water (25 ml) with varying polymer concentrations were prepared by quasi-emulsion solvent diffusion method and evaluated for % Production Yield, % drug content, % encapsulation efficiency, particle size, polydispersity index (PDI) and % drug release characteristics. The selected Microsponges formulation (F3) was incorporated in Carpopol 934 gel for topical application. The prepared gel (CLRMS-F3 Gel) was evaluated for physical characteristics, pH, spreadability, viscosity, and in vitro drug release. Furthermore, the gel formulation was compared with pure clarithromycin gel for antibacterial activity against Gram positive stain (S. aureus) and Gram negative (E. coli.) by cup and plate method. The F3 microsponge formulation exhibited a production yield of 83.75%, drug content (21.5 ± 0.50 %), encapsulation efficiency of 86.04 ± 2.30%. Their particle size was satisfactory (3.80 ± 0.01 µm) and they were found to be spherical and porous in nature. F3 microsponges released 69.36 ± 1.27 % of the drug over a period of 8 hrs and were incorporated into the gel formulations. The gel prepared using F3 microsponges was transparent, homogenous and exhibited pH of 6.8 ± 0.02, Spreadability 9.92 ± 0.44 g/cm and viscosity 35370.17 ± 493.09 centipoise. The CLRMS-F3 gel released 82.13 ± 0.47 % drug in 12 hrs by zero-order kinetic. The antibacterial activity studies revealed a higher potency against both S. aureus and E. coli of the prepared CLRMS-F3 gel in comparison to both pure CLR gel and azithromycin standard. On the basis of the above study, it may be concluded that microsponges gel formulation can be potentially useful in improving topical drug delivery of antibacterial agents and can give better therapeutic efficacy.
{"title":"Formulation, Characterization and Antibacterial Study of Microsponges Loaded Gel of Clarithromycin for Topical Drug Delivery","authors":"Mohit Kumar Tomar, S. Pahwa, L. Tyagi, C. Gupta, Preeti Maan, V. Sethi","doi":"10.2174/2210303112666220412134241","DOIUrl":"https://doi.org/10.2174/2210303112666220412134241","url":null,"abstract":"\u0000\u0000Microsponge drug delivery systems comprise of spherical and porous microspheres used for prolonged topical drug delivery. These systems considerably reduce the undesirable side effects, offering improved patient compliance and reduced dosing frequency.\u0000\u0000\u0000\u0000The present study was focused on the development of topical controlled release preparations of microsponges loaded gel of clarithromycin with the purpose to cure bacterial skin infections.\u0000\u0000\u0000\u0000Four batches of Microsponges (F1, F2, F3, and F4) of clarithromycin (CLR) containing fixed amounts of clarithromycin (100 mg), Dichloromethane (5 ml), polyvinyl alcohol (5 % w/v) and distilled water (25 ml) with varying polymer concentrations were prepared by quasi-emulsion solvent diffusion method and evaluated for % Production Yield, % drug content, % encapsulation efficiency, particle size, polydispersity index (PDI) and % drug release characteristics. The selected Microsponges formulation (F3) was incorporated in Carpopol 934 gel for topical application. The prepared gel (CLRMS-F3 Gel) was evaluated for physical characteristics, pH, spreadability, viscosity, and in vitro drug release. Furthermore, the gel formulation was compared with pure clarithromycin gel for antibacterial activity against Gram positive stain (S. aureus) and Gram negative (E. coli.) by cup and plate method.\u0000\u0000\u0000\u0000The F3 microsponge formulation exhibited a production yield of 83.75%, drug content (21.5 ± 0.50 %), encapsulation efficiency of 86.04 ± 2.30%. Their particle size was satisfactory (3.80 ± 0.01 µm) and they were found to be spherical and porous in nature. F3 microsponges released 69.36 ± 1.27 % of the drug over a period of 8 hrs and were incorporated into the gel formulations. The gel prepared using F3 microsponges was transparent, homogenous and exhibited pH of 6.8 ± 0.02, Spreadability 9.92 ± 0.44 g/cm and viscosity 35370.17 ± 493.09 centipoise. The CLRMS-F3 gel released 82.13 ± 0.47 % drug in 12 hrs by zero-order kinetic. The antibacterial activity studies revealed a higher potency against both S. aureus and E. coli of the prepared CLRMS-F3 gel in comparison to both pure CLR gel and azithromycin standard.\u0000\u0000\u0000\u0000On the basis of the above study, it may be concluded that microsponges gel formulation can be potentially useful in improving topical drug delivery of antibacterial agents and can give better therapeutic efficacy.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44355641","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-30DOI: 10.2174/2210303112666220330115110
Yee Chu Kwa, Theebaa Anasamy, Y. Foo, B. Leo, I. Chung, L. Kiew, L. Chung
Stattic offers a unique inhibitory effect on the STAT3 signaling pathway, a crucial mechanism in the progression of metastatic cancer. However, the development of Stattic has been impeded by its hydrophobicity and lack of specificity. To overcome these limitations, encapsulation of Stattic with polymeric micelles was previously attempted, which led to a significant increase in the potency of Stattic on breast cancer cell lines. The presence of albumin was believed to contribute to such enhancement, as the protein corona layer formation helps to retain the micellar structure before eventual uptake by the cells. Moreover, a previous study had reported the unique affinity of Stattic towards albumin molecule. This study aimed to explore the integration of Stattic in albumin-based nanoparticles and to assess the in vitro effects. Albumin/Stattic nanoparticles were prepared by crosslinking with glutaraldehyde. The yielded nanoparticles were 150.0 ± 6.6 nm in size, with ~53% entrapment efficiency. The cumulative release of Stattic in a tumoric acidic environment (pH 5.3; 59%) was 2.6-fold more than neutral environment (pH 7.4; 23%). In blood plasma, 7% cumulative release was observed. The mathematical modeling of the release kinetics revealed that the albumin/Stattic nanoparticles in phosphate buffer saline and plasma followed Korsmeyer-Peppas and Higuchi model, respectively. Among the two cell lines tested, metastatic MDA-MB-231 cells were more sensitive to entrapment of Stattic with albumin nanoparticles, as the IC50 value decreased by 2.5-fold compared to free Stattic. This study reports the formation of low immunogenic and cost-efficient albumin nanoparticles to improve the delivery of Stattic.
{"title":"Preparation and Characterization of Stattic-Loaded Albumin Nanoparticles for Antimetastatic Cancer Treatment","authors":"Yee Chu Kwa, Theebaa Anasamy, Y. Foo, B. Leo, I. Chung, L. Kiew, L. Chung","doi":"10.2174/2210303112666220330115110","DOIUrl":"https://doi.org/10.2174/2210303112666220330115110","url":null,"abstract":"\u0000\u0000Stattic offers a unique inhibitory effect on the STAT3 signaling pathway, a crucial mechanism in the progression of metastatic cancer. However, the development of Stattic has been impeded by its hydrophobicity and lack of specificity. To overcome these limitations, encapsulation of Stattic with polymeric micelles was previously attempted, which led to a significant increase in the potency of Stattic on breast cancer cell lines. The presence of albumin was believed to contribute to such enhancement, as the protein corona layer formation helps to retain the micellar structure before eventual uptake by the cells. Moreover, a previous study had reported the unique affinity of Stattic towards albumin molecule.\u0000\u0000\u0000\u0000This study aimed to explore the integration of Stattic in albumin-based nanoparticles and to assess the in vitro effects.\u0000\u0000\u0000\u0000Albumin/Stattic nanoparticles were prepared by crosslinking with glutaraldehyde.\u0000\u0000\u0000\u0000The yielded nanoparticles were 150.0 ± 6.6 nm in size, with ~53% entrapment efficiency. The cumulative release of Stattic in a tumoric acidic environment (pH 5.3; 59%) was 2.6-fold more than neutral environment (pH 7.4; 23%). In blood plasma, 7% cumulative release was observed. The mathematical modeling of the release kinetics revealed that the albumin/Stattic nanoparticles in phosphate buffer saline and plasma followed Korsmeyer-Peppas and Higuchi model, respectively. Among the two cell lines tested, metastatic MDA-MB-231 cells were more sensitive to entrapment of Stattic with albumin nanoparticles, as the IC50 value decreased by 2.5-fold compared to free Stattic.\u0000\u0000\u0000\u0000This study reports the formation of low immunogenic and cost-efficient albumin nanoparticles to improve the delivery of Stattic.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43674438","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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