Pub Date : 2022-11-22DOI: 10.2174/2210303113666221122113514
Dilpreet K Singh, Russel Tonjam, B. Kurmi
The present investigation aims to develop a solid Self-nano emulsifying Drug Delivery System for enhancing the solubility and in vitro characteristics of poorly soluble anti-hypertensive drug Bosentan Monohydrate. The selection of formulation components on the basis of equilibrium solubility and pseudo-ternary phase titration studies revealed the suitability of Isopropyl myristate, Tween 80 and Polyethylene glycol as the lipidic excipients and their optimized concentration ranges resulted in a stable microemulsion region. The systematic optimization of the liquid SNEDD formulations of Bosentan was performed using in vitro tests and detailed characterization studies. The results revealed that the F4 formulation produces excellent results and satisfactory results in all the CQA of liquid SNEDDS. The optimized liquid SNEDD formulations exhibited globule size of less than 100 nm, high and negative values of zeta potential, quick self-emulsification rate, negligible phase separation, and a high degree of physical stability during thermodynamic evaluation studies. SEM revealed nanostructured particles with negligible aggregation. In vitro dissolution studies of Bosentan in optimized liquid SNEDDS (F4) unveiled a multi-fold enhancement in release profile, as compared to pure API.
{"title":"Development and Characterization of Bosentan Monohydrate-loaded\u0000Self-Nano Emulsifying Drug Delivery System","authors":"Dilpreet K Singh, Russel Tonjam, B. Kurmi","doi":"10.2174/2210303113666221122113514","DOIUrl":"https://doi.org/10.2174/2210303113666221122113514","url":null,"abstract":"\u0000\u0000The present investigation aims to develop a solid Self-nano emulsifying\u0000Drug Delivery System for enhancing the solubility and in vitro characteristics of poorly soluble anti-hypertensive drug Bosentan Monohydrate.\u0000\u0000\u0000\u0000The selection of formulation components on the basis of equilibrium solubility and pseudo-ternary phase titration studies revealed the suitability of Isopropyl myristate, Tween 80 and Polyethylene glycol as the lipidic excipients and their optimized concentration ranges resulted in a stable microemulsion region.\u0000\u0000\u0000\u0000The systematic optimization of the liquid SNEDD formulations of Bosentan was performed using in vitro tests and detailed characterization studies. The results revealed that the F4\u0000formulation produces excellent results and satisfactory results in all the CQA of liquid SNEDDS.\u0000The optimized liquid SNEDD formulations exhibited globule size of less than 100 nm, high and\u0000negative values of zeta potential, quick self-emulsification rate, negligible phase separation, and a\u0000high degree of physical stability during thermodynamic evaluation studies. SEM revealed\u0000nanostructured particles with negligible aggregation.\u0000\u0000\u0000\u0000In vitro dissolution studies of Bosentan in optimized liquid SNEDDS (F4) unveiled a\u0000multi-fold enhancement in release profile, as compared to pure API.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41645791","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 : 2022-11-17DOI: 10.2174/2210303113666221117085703
M. Ahuja, Preeti Chauhan, Rimpy, P. Kumari, T. Kumar
Topical therapy for nail infection has a serious drawback of drug permeation via keratinized human nail plate. Onychomycosis, or tinea unguium, is a human nail fungal infection affecting nearly 19% of the world’s population. Purposely, we aimed to develop and evaluate nail lacquer formulations incorporated with luliconazole utilizing different permeation enhancers for targeted transungual drug delivery. Nail clippings were treated with luliconazole solution (5% w/v) with or without permeation enhancers and screened by determining the hydration enhancement factor and retention of the drug in the nail clippings. Different batches of nail lacquer formulations were prepared to employ Eudragit, polyethylene glycol 400, Tween 80, and permeation enhancer with the highest hydration enhancement factor value. Successively, the formulations were evaluated for studies like compatibility, application, gloss, blush, smoothness of flow, adhesion, non-volatile content, etc. Based on the results of physical characterization and in vitro release study, formulations based on Eudragit RLPO and RSPO containing N-acetylcysteine and urea and the Eudragit RL100 containing urea as penetration enhancer were found to be potentially useful. Furthermore, a comparative ex vivo evaluation of the formulations for permeation across the nail clippings revealed that the luliconazole-loaded Eudragit RLPO formulations containing N-acetylcysteine and urea provided the highest flux (5.12 µg/cm2/min) and shortest lag time (17.4 min). Morphological analysis showed an increase in the number of pores on the nail surface, leading to the enhancement of drug diffusion across the nail matrix and nail bed. Furthermore, the luliconazole nail lacquer formulation exhibited higher antifungal activity, viscosity, and stability properties. Hence, the results suggest that the developed luliconazole nail lacquer formulation is an efficient topical transungual drug delivery system.
{"title":"Development and Evaluation of Luliconazole Nail Lacquer Containing Potential Permeation Enhancers for an Enhanced Transungual Drug Delivery","authors":"M. Ahuja, Preeti Chauhan, Rimpy, P. Kumari, T. Kumar","doi":"10.2174/2210303113666221117085703","DOIUrl":"https://doi.org/10.2174/2210303113666221117085703","url":null,"abstract":"\u0000\u0000Topical therapy for nail infection has a serious drawback of drug permeation via keratinized human nail plate. Onychomycosis, or tinea unguium, is a human nail fungal infection affecting nearly 19% of the world’s population.\u0000\u0000\u0000\u0000Purposely, we aimed to develop and evaluate nail lacquer formulations incorporated with luliconazole utilizing different permeation enhancers for targeted transungual drug delivery. Nail clippings were treated with luliconazole solution (5% w/v) with or without permeation enhancers and screened by determining the hydration enhancement factor and retention of the drug in the nail clippings. Different batches of nail lacquer formulations were prepared to employ Eudragit, polyethylene glycol 400, Tween 80, and permeation enhancer with the highest hydration enhancement factor value.\u0000\u0000\u0000\u0000Successively, the formulations were evaluated for studies like compatibility, application, gloss, blush, smoothness of flow, adhesion, non-volatile content, etc. Based on the results of physical characterization and in vitro release study, formulations based on Eudragit RLPO and RSPO containing N-acetylcysteine and urea and the Eudragit RL100 containing urea as penetration enhancer were found to be potentially useful. Furthermore, a comparative ex vivo evaluation of the formulations for permeation across the nail clippings revealed that the luliconazole-loaded Eudragit RLPO formulations containing N-acetylcysteine and urea provided the highest flux (5.12 µg/cm2/min) and shortest lag time (17.4 min).\u0000\u0000\u0000\u0000Morphological analysis showed an increase in the number of pores on the nail surface, leading to the enhancement of drug diffusion across the nail matrix and nail bed.\u0000\u0000\u0000\u0000Furthermore, the luliconazole nail lacquer formulation exhibited higher antifungal activity, viscosity, and stability properties. Hence, the results suggest that the developed luliconazole nail lacquer formulation is an efficient topical transungual drug delivery system.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42677080","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 : 2022-11-03DOI: 10.2174/2210303113666221103104829
S. Bhatt, P. Mathur, R. Verma, Manish Kumar, V. Jhawat, R. Dutt
Rheumatoid arthritis (RA) is a well-known chronic inflammatory disease that results in articular degradation, comorbidities, and body part functional loss. In the last two decades, the development of effective biologics and small compounds, such as Janus kinase inhibitors (Jakinibs), has significantly improved clinical outcomes. Low-molecular-weight chemicals known as jakinibs are currently used for effective treatment of RA. Jakinibs are a new class of drugs being developed to treat RA, and several of them are now in different phases of clinical trials to establish their safety and efficacy in humans. Jakinibs can be very different in their selectivity against JAK inhibitors. For an efficient therapy of RA, it is critical to fully comprehend the properties of JAK inhibitors as well as their mechanism of action. Tofacitinib, Baricitinib, Upadacitinib, Peficitinib, Filgotinib, Decernotinib, Itacitinib, Ruxolitinib, and PF-06651600 are a few selective orally active Jakinibs that have entered clinical trials to treat RA. This review aims to elaborate on Jakinibs for the treatment of Rheumatoid Arthritis (RH), including their mechanism of action (MOA), efficacy and safety profiles, clinical trials of adverse effects (AEs) associated with Jakinibs and combination therapy with other DMARDs.
{"title":"Current remedial strategies for the treatment of rheumatoid arthritis through the oral route with Janus kinase inhibitors","authors":"S. Bhatt, P. Mathur, R. Verma, Manish Kumar, V. Jhawat, R. Dutt","doi":"10.2174/2210303113666221103104829","DOIUrl":"https://doi.org/10.2174/2210303113666221103104829","url":null,"abstract":"\u0000\u0000Rheumatoid arthritis (RA) is a well-known chronic inflammatory disease that results in\u0000articular degradation, comorbidities, and body part functional loss. In the last two decades, the development of effective biologics and small compounds, such as Janus kinase inhibitors (Jakinibs),\u0000has significantly improved clinical outcomes. Low-molecular-weight chemicals known as jakinibs\u0000are currently used for effective treatment of RA. Jakinibs are a new class of drugs being developed\u0000to treat RA, and several of them are now in different phases of clinical trials to establish their safety\u0000and efficacy in humans. Jakinibs can be very different in their selectivity against JAK inhibitors.\u0000For an efficient therapy of RA, it is critical to fully comprehend the properties of JAK inhibitors as\u0000well as their mechanism of action. Tofacitinib, Baricitinib, Upadacitinib, Peficitinib, Filgotinib, Decernotinib, Itacitinib, Ruxolitinib, and PF-06651600 are a few selective orally active Jakinibs that\u0000have entered clinical trials to treat RA. This review aims to elaborate on Jakinibs for the treatment\u0000of Rheumatoid Arthritis (RH), including their mechanism of action (MOA), efficacy and safety profiles, clinical trials of adverse effects (AEs) associated with Jakinibs and combination therapy with\u0000other DMARDs.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48503616","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 : 2022-09-29DOI: 10.2174/2210303112666220929151010
Rashmi Singh, P. Gaur, Sameer Rastogi, K. Lata
Phytopharmaceuticals are herbal medicines that include standardized extracts, bioactive fractions, and purified phytoconstituents. They have been used for the cure, treatment, and mitigation of diseases since ancient times. Phytopharmaceuticals have a wide array of health benefits but their therapeutic efficacy is limited due to poor absorption, low bioavailability, and early elimination profile. A novel phospholipid complex is a newly introduced patented technology initially developed to incorporate standardized plant extracts/fractions or water-soluble phytoconstituents into phospholipids to produce a lipid compatible molecular complex, called phytosome, which improves their absorption and bioavailability. In herbal formulations, phytosome is the most advanced dosage form that has upgraded absorption rate and improved pharmacokinetics in comparison with conventional products. Phospholipid-complex is the result of hydrogen bonding between phospholipids and phytoconstituents, which offers maximum incorporation of herbal active ingredients into the lipidic layer and core. The increased therapeutic efficacy is due to the formation of amphiphilic phospholipid complex of herbal medicine. This review highlights the role of phospholipids in the delivery of herbal bioactives and natural extracts with special emphasis on phytosomes. Moreover, the current status of bioavailabilities, commercial products, patents, and clinical trials of phytosomal system of phytopharmaceuticals were addressed.
{"title":"Recent advancements and applications of phospholipid complexes – A strategy to enhancing the bioavailability of phytopharmaceuticals","authors":"Rashmi Singh, P. Gaur, Sameer Rastogi, K. Lata","doi":"10.2174/2210303112666220929151010","DOIUrl":"https://doi.org/10.2174/2210303112666220929151010","url":null,"abstract":"\u0000\u0000Phytopharmaceuticals are herbal medicines that include standardized extracts, bioactive fractions, and purified phytoconstituents. They have been used for the cure, treatment, and mitigation of diseases since ancient times. Phytopharmaceuticals have a wide array of health benefits but their therapeutic efficacy is limited due to poor absorption, low bioavailability, and early elimination profile. A novel phospholipid complex is a newly introduced patented technology initially developed to incorporate standardized plant extracts/fractions or water-soluble phytoconstituents into phospholipids to produce a lipid compatible molecular complex, called phytosome, which improves their absorption and bioavailability. In herbal formulations, phytosome is the most advanced dosage form that has upgraded absorption rate and improved pharmacokinetics in comparison with conventional products. Phospholipid-complex is the result of hydrogen bonding between phospholipids and phytoconstituents, which offers maximum incorporation of herbal active ingredients into the lipidic layer and core. The increased therapeutic efficacy is due to the formation of amphiphilic phospholipid complex of herbal medicine. This review highlights the role of phospholipids in the delivery of herbal bioactives and natural extracts with special emphasis on phytosomes. Moreover, the current status of bioavailabilities, commercial products, patents, and clinical trials of phytosomal system of phytopharmaceuticals were addressed.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44013907","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 : 2022-09-07DOI: 10.2174/2210303112666220907124554
E. R. Rani, G. Radha
The current study explores the enhancement of solubility and dissolution rate of a poorly water-soluble drug Iloperidone (IPD) by synthesizing co-crystals (CC) using 4- amino benzoic acid (ABA) as a coformer. Pharmaceutical CCs of IPD with ABA were designed and synthesized using crystal engineering. CCs were prepared by solvent evaporation (SE) technique and studied for their enhancement in solubility and dissolution rate. CC formation was confirmed by Fourier Transform InfraRed Spectroscopy (FTIR), powder X-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), and Proton Nuclear Magnetic Resonance (1H- NMR) Structural characterization studies exhibited new characteristic peaks, which confirmed that CCs could be generated from IPD and ABA using SE technique. The apparent aqueous solubility studies of the CCs exhibited 7.1 folds increase in solubility compared to the pure drug. Improvement in the rate of dissolution of CCs was evident from the in vitro dissolution studies, where CCs displayed 94.15 ± 0.27% drug release in 60min while pure drug showed only 39.90 ± 1.86% release in the same time period CCs of IPD and ABA provide a novel approach to overcoming the solubility issues.
{"title":"Tailoring Physicochemical Properties of Iloperidone by Cocrystallization:\u0000Design and Characterization of Novel Cocrystals of Iloperidone and 4-\u0000amino Benzoic Acid","authors":"E. R. Rani, G. Radha","doi":"10.2174/2210303112666220907124554","DOIUrl":"https://doi.org/10.2174/2210303112666220907124554","url":null,"abstract":"\u0000\u0000The current study explores the enhancement of solubility and dissolution\u0000rate of a poorly water-soluble drug Iloperidone (IPD) by synthesizing co-crystals (CC) using 4-\u0000amino benzoic acid (ABA) as a coformer.\u0000\u0000\u0000\u0000Pharmaceutical CCs of IPD with ABA were designed and synthesized using crystal engineering. CCs were prepared by solvent evaporation (SE) technique and studied for their enhancement in solubility and dissolution rate. CC formation was confirmed by Fourier Transform InfraRed Spectroscopy (FTIR), powder X-ray diffraction (PXRD), Differential Scanning Calorimetry\u0000(DSC), and Proton Nuclear Magnetic Resonance (1H- NMR)\u0000\u0000\u0000\u0000Structural characterization studies exhibited new characteristic peaks, which confirmed\u0000that CCs could be generated from IPD and ABA using SE technique. The apparent aqueous solubility studies of the CCs exhibited 7.1 folds increase in solubility compared to the pure drug. Improvement in the rate of dissolution of CCs was evident from the in vitro dissolution studies, where\u0000CCs displayed 94.15 ± 0.27% drug release in 60min while pure drug showed only 39.90 ± 1.86%\u0000release in the same time period\u0000\u0000\u0000\u0000CCs of IPD and ABA provide a novel approach to overcoming the solubility issues.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43034836","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 : 2022-08-31DOI: 10.2174/2210303112666220831100748
A. Mneimneh, H. El-Maradny
The pulmonary route of administration has shown viability and effectiveness in local and systemic delivery, as a non-invasive method, not only for active pharmaceutical ingredients but also for genes, proteins, and enzymes for pulmonary and non-pulmonary diseases. Nanoparticulate systems such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, emulsions, nanosuspensions, polymeric nanoparticles, and metal-based have been investigated as delivery carriers for the lungs. Nanoparticulate drug delivery systems are known for their optimum small size and suitability for pulmonary absorption as it is well recognized that drug particles within the size range of 1–5 μm are the best for pulmonary deposition. The advantages of these colloidal systems are generated by their small size, large surface area, and rapid absorption. These systems are characterized by ease of preparation as inhalable formulation, the ability to increase drug concentration at the site of disease, preventing and minimizing drug loss and degradation, and the possibility of cell targeting. This article provides a brief review of the features of different aerosol devices, their advantages, limitations, and methods utilized for particle size analysis with a focus on the emerging field of nanocarriers as vehicles for pulmonary delivery for various lung disorders.
{"title":"A Review on Aerosol Drug Delivery: Fundamentals, Classifications, Particle Size Analysis and the Engagement of Nanoparticulate Systems","authors":"A. Mneimneh, H. El-Maradny","doi":"10.2174/2210303112666220831100748","DOIUrl":"https://doi.org/10.2174/2210303112666220831100748","url":null,"abstract":"\u0000\u0000The pulmonary route of administration has shown viability and effectiveness in local and systemic delivery, as a non-invasive method, not only for active pharmaceutical ingredients but also for genes, proteins, and enzymes for pulmonary and non-pulmonary diseases.\u0000\u0000\u0000\u0000Nanoparticulate systems such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, emulsions, nanosuspensions, polymeric nanoparticles, and metal-based have been investigated as delivery carriers for the lungs. Nanoparticulate drug delivery systems are known for their optimum small size and suitability for pulmonary absorption as it is well recognized that drug particles within the size range of 1–5 μm are the best for pulmonary deposition.\u0000\u0000\u0000\u0000The advantages of these colloidal systems are generated by their small size, large surface area, and rapid absorption. These systems are characterized by ease of preparation as inhalable formulation, the ability to increase drug concentration at the site of disease, preventing and minimizing drug loss and degradation, and the possibility of cell targeting.\u0000\u0000\u0000\u0000This article provides a brief review of the features of different aerosol devices, their advantages, limitations, and methods utilized for particle size analysis with a focus on the emerging field of nanocarriers as vehicles for pulmonary delivery for various lung disorders.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41460589","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 : 2022-08-29DOI: 10.2174/2210303112666220829125054
F. Dorkoosh, S. Handali, I. Haririan, M. Vaziri
Coronavirus disease (COVID-19) is an infectious disease caused by coronavirus. Developing specific drugs for inhibiting replication and viral entry is crucial. Several clinical trial studies are underway to evaluate the efficacy of anti-viral drugs for COVID-19 patients. Nanomedicine formulations can present a novel strategy for targeting the virus life cycle. Nano-drug delivery systems can modify the pharmacodynamics and pharmacokinetics properties of anti-viral drugs and reduce their adverse effects. Moreover, nanocarriers can directly exhibit anti-viral effects. A number of nanocarriers have been studied for this purpose, including liposomes, dendrimers, exosomes and decoy nanoparticles (NPs). Among them, decoy NPs have been considered more as nanodecoys can efficiently protect host cells from the infection of SARS-CoV-2. The aim of this review article is to highlight the probable nanomedicine therapeutic strategies to develop anti-viral drug delivery systems for the treatment of COVID-19.
{"title":"Nanomedicine “New Food for an Old Mouth”: Novel Approaches for the\u0000Treatment of COVID-19","authors":"F. Dorkoosh, S. Handali, I. Haririan, M. Vaziri","doi":"10.2174/2210303112666220829125054","DOIUrl":"https://doi.org/10.2174/2210303112666220829125054","url":null,"abstract":"\u0000\u0000Coronavirus disease (COVID-19) is an infectious disease caused by coronavirus. Developing specific drugs for inhibiting replication and viral entry is crucial. Several clinical trial studies\u0000are underway to evaluate the efficacy of anti-viral drugs for COVID-19 patients. Nanomedicine\u0000formulations can present a novel strategy for targeting the virus life cycle. Nano-drug delivery systems can modify the pharmacodynamics and pharmacokinetics properties of anti-viral drugs and reduce their adverse effects. Moreover, nanocarriers can directly exhibit anti-viral effects. A number\u0000of nanocarriers have been studied for this purpose, including liposomes, dendrimers, exosomes and\u0000decoy nanoparticles (NPs). Among them, decoy NPs have been considered more as nanodecoys can\u0000efficiently protect host cells from the infection of SARS-CoV-2. The aim of this review article is to\u0000highlight the probable nanomedicine therapeutic strategies to develop anti-viral drug delivery systems for the treatment of COVID-19.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49555289","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 : 2022-08-18DOI: 10.2174/2210303112666220818115231
P. Pandey, N. Minocha, N. Vashist, Rashmi Shah, Sapna Saini, Manish Makhija, Deepika Purohit, D. Kaushik
During the development of the new formulations, the hydrophobic drugs face many problems leading to poor water solubility and problems related to bioavailability. Topical drug delivery is a popular and unique process that directs the action of various drugs on the skin for the treatment and diagnosis of various diseases and disorders such as urticaria, inflammation, rheumatism, etc. This topical release system is usually used to escape the first-pass metabolism. An emulgel is a superior formulation with combined advantages of both an emulsion and agel. Gel preparations normally offer earlier drug release than other predictable ointments and creams. The main aim of this review is to deal with the problems associated with the delivery of hydrophobic drugs and to tackle these problems using an emulgel formulation. Emulgel mainly provides better stability, prolonged local contact, controlled release of drugs with short half-life, and better loading capacity. The review was extracted from the searches performed in PubMed, Google Patents, Medline, and Google Scholars, etc. Data from these searches were collected and evaluated to get information about the available literature on the emulgel formulation. The literature obtained was studied thoroughly as per the requirement of the objective of this review. The details of the emulgel formulation, the advantages and disadvantages associated with it, and the methods for characterization of the formulation are compiled here in this review. Along with this, some reported patents have also been included in this review to conclude the future of emulgel formulation in topical drug delivery. Emulgel is becoming very popular as a drug delivery system to deliver many antifungal, analgesics, anti-acne, anti-inflammatory drugs, and a number of cosmetics with a wide scope to be explored further. This review article is motivated by the formulation, characterization, patents, and biological activities of emulgel formulation.
{"title":"Emulgel: An Emerging Approach towards Effective Topical Drug Delivery","authors":"P. Pandey, N. Minocha, N. Vashist, Rashmi Shah, Sapna Saini, Manish Makhija, Deepika Purohit, D. Kaushik","doi":"10.2174/2210303112666220818115231","DOIUrl":"https://doi.org/10.2174/2210303112666220818115231","url":null,"abstract":"\u0000\u0000During the development of the new formulations, the hydrophobic drugs\u0000face many problems leading to poor water solubility and problems related to bioavailability. Topical\u0000drug delivery is a popular and unique process that directs the action of various drugs on the skin for\u0000the treatment and diagnosis of various diseases and disorders such as urticaria, inflammation, rheumatism, etc. This topical release system is usually used to escape the first-pass metabolism. An\u0000emulgel is a superior formulation with combined advantages of both an emulsion and agel. Gel\u0000preparations normally offer earlier drug release than other predictable ointments and creams.\u0000\u0000\u0000\u0000The main aim of this review is to deal with the problems associated with the delivery of\u0000hydrophobic drugs and to tackle these problems using an emulgel formulation. Emulgel mainly\u0000provides better stability, prolonged local contact, controlled release of drugs with short half-life, and\u0000better loading capacity.\u0000\u0000\u0000\u0000The review was extracted from the searches performed in PubMed, Google Patents, Medline, and Google Scholars, etc. Data from these searches were collected and evaluated to get information about the available literature on the emulgel formulation. The literature obtained was studied\u0000thoroughly as per the requirement of the objective of this review.\u0000\u0000\u0000\u0000The details of the emulgel formulation, the advantages and disadvantages associated with\u0000it, and the methods for characterization of the formulation are compiled here in this review. Along\u0000with this, some reported patents have also been included in this review to conclude the future of\u0000emulgel formulation in topical drug delivery.\u0000\u0000\u0000\u0000Emulgel is becoming very popular as a drug delivery system to deliver many antifungal, analgesics, anti-acne, anti-inflammatory drugs, and a number of cosmetics with a wide scope to\u0000be explored further. This review article is motivated by the formulation, characterization, patents,\u0000and biological activities of emulgel formulation.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48314309","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 : 2022-08-17DOI: 10.2174/2210303112666220817100319
Chandir C. Ramani, R. J. Babu, M. Dhanasekaran, S. Apte, D. Rambhau
Amidst levodopa being considered as the “Gold standard” in the treatment of Parkinson’s disease (PD), it still has critical therapeutic issues with its dose regimen and dosage forms leading to severe adverse drug effects, decreased drug efficacy during chronic use, and requires an enforced “drug holiday” in PD patients. Hence, in this study, we designed a novel levodopa and carbidopa water-in-oil-in-water (w/o/w) formulation for bioavailability improvement in the central nervous system (CNS). The new one-in-one embedment of the w/o/w levodopa and carbidopa emulsion formulation was obtained by a double emulsion technique. The plasma and brain levels following intravenous administration of the emulsions in rats were determined. The incorporation of stearylamine (a cationic surfactant) considerably increased the surface charge density of the emulsion droplets. This formulation exhibited a narrow particle size distribution enabling parenteral administration. The formulation also provided a high drug loading capacity. In in vivo study, this novel formulation significantly increased the bioavailability of levodopa in the CNS (P < 0.001). The strong resistance to desorption (due to higher charge density) and the presence of positive charge on the particles upon dilution may be the main reason for enhanced brain levels of levodopa. Our current formulation F5 may decrease the dose of levodopa, leading to decreased adverse effects and dosing problems, thus appreciably benefit PD patients in the future.
{"title":"Effect of surface charge density of a w/o/w emulsion on the brain targeting of levodopa in Rats for the treatment of Parkinson’s Disease","authors":"Chandir C. Ramani, R. J. Babu, M. Dhanasekaran, S. Apte, D. Rambhau","doi":"10.2174/2210303112666220817100319","DOIUrl":"https://doi.org/10.2174/2210303112666220817100319","url":null,"abstract":"\u0000\u0000Amidst levodopa being considered as the “Gold standard” in the treatment\u0000of Parkinson’s disease (PD), it still has critical therapeutic issues with its dose regimen and dosage\u0000forms leading to severe adverse drug effects, decreased drug efficacy during chronic use, and requires an enforced “drug holiday” in PD patients. Hence, in this study, we designed a novel levodopa and carbidopa water-in-oil-in-water (w/o/w) formulation for bioavailability improvement in the\u0000central nervous system (CNS).\u0000\u0000\u0000\u0000The new one-in-one embedment of the w/o/w levodopa and carbidopa emulsion formulation was obtained by a double emulsion technique. The plasma and brain levels following intravenous administration of the emulsions in rats were determined.\u0000\u0000\u0000\u0000The incorporation of stearylamine (a cationic surfactant) considerably increased the surface\u0000charge density of the emulsion droplets. This formulation exhibited a narrow particle size distribution enabling parenteral administration. The formulation also provided a high drug loading capacity.\u0000In in vivo study, this novel formulation significantly increased the bioavailability of levodopa in the\u0000CNS (P < 0.001). The strong resistance to desorption (due to higher charge density) and the presence of positive charge on the particles upon dilution may be the main reason for enhanced brain\u0000levels of levodopa.\u0000\u0000\u0000\u0000Our current formulation F5 may decrease the dose of levodopa, leading to decreased\u0000adverse effects and dosing problems, thus appreciably benefit PD patients in the future.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44464894","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 : 2022-08-04DOI: 10.2174/2210303112666220804102050
A. Puri, Vrushali Gokhale
The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation. The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch. Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia. From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.
{"title":"Isolation, Characterization of Banana Starch and its Evaluation as a Disintegrating agent in Dispersible Lornoxicam Tablet","authors":"A. Puri, Vrushali Gokhale","doi":"10.2174/2210303112666220804102050","DOIUrl":"https://doi.org/10.2174/2210303112666220804102050","url":null,"abstract":"\u0000\u0000The present study was designed to isolate, characterize, formulate, and evaluate the disintegration properties of banana starch in dispersible Lornoxicam tablet formulation.\u0000\u0000\u0000\u0000The alkaline extraction method used sodium hydroxide as a lye solution to isolate starch from unripe banana fruit. Starch was subjected to characterization for physicochemical properties, viscosity and flow properties, Fourier-transform infrared spectroscopy (FTIR) scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray crystallography (XRD) study. Flow properties of starch were determined as per the standard procedure. Tablets were formulated by a wet granulation method using starch as a disintegrant, and the in-vitro release characteristic of the prepared tablets was analyzed. Different concentrations of isolated starch were studied for disintegrating properties compared to corn starch.\u0000\u0000\u0000\u0000Studies indicate that starch obtained is qualitatively and quantitatively comparable to corn starch. SEM, FTIR, DSC and XRD data confirmed the polysaccharide nature of the starch. The physicochemical properties of starch passed the prescribed evaluation tests for tablets. These tablets also confirmed the disintegration and dissolution specifications as per Indian Pharmacopoeia.\u0000\u0000\u0000\u0000From the above study, it can be concluded that starch obtained from banana shows qualitatively and quantitatively good disintegration characteristics compared to corn starch. These tablets also confirmed a significant degree of dissolution as per the standards. Evaluations also specified that banana starch possesses acceptable disintegrating characteristics compared to corn starch and can be used as a disintegrant in tablet formulation.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49254296","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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