Pub Date : 2021-08-31DOI: 10.2174/2210303111666210831170312
V. Suryawanshi, K. Sarwa, S. N. Sakarkar, C. Kaur
Rosuvastatin calcium is a statin class of drug having limited oral bioavailability of about 20%. This problem might be overcome by making the biform complex using cow ghee fraction as a bioavailability enhancer. A precise thermal fractionation technique was adopted to separate different fatty acids from cow ghee. Collected fractions were subjected to characterization over parameters reported for fatty acids. LC-MS and FTIR confirm the content variation in the collected fraction. Biform complex was prepared by fusion method with a constant ratio of drug and cow ghee fraction. The prepared complex was subjected to FTIR, DSC, and LC-MS study to confirm chemical composition characteristics. Drug content, in-vitro and ex-vivo permeation studies were also performed. The anti-inflammatory response was measured using the carrageenan paw-induced edema rat model. Lipid-lowering effect and inflammation marker analysis was also performed using ELISA specific kit. The biform complex prepared with a thermal fraction at 30ºC of cow ghee show the highest in-vitro and ex-vivo permeation. The anti-inflammation response of the biform complex F1 was higher than other tested formulations with considerable lipid and lipoprotein lowering properties. This study confirms that the thermal fractionation method abled to separate cow ghee as per their fatty acid content. The complexion of rosuvastatin calcium with cow ghee thermal fraction enhances oral bioavailability followed by the anti-inflammatory and lipid-lowering activity.
{"title":"A novel rosuvastatin calcium cow ghee fraction biform complex: formulation characterization and evaluation","authors":"V. Suryawanshi, K. Sarwa, S. N. Sakarkar, C. Kaur","doi":"10.2174/2210303111666210831170312","DOIUrl":"https://doi.org/10.2174/2210303111666210831170312","url":null,"abstract":"\u0000\u0000Rosuvastatin calcium is a statin class of drug having limited oral bioavailability of about 20%. This problem might be overcome by making the biform complex using cow ghee fraction as a bioavailability enhancer. \u0000\u0000\u0000\u0000\u0000 A precise thermal fractionation technique was adopted to separate different fatty acids from cow ghee. Collected fractions were subjected to characterization over parameters reported for fatty acids. LC-MS and FTIR confirm the content variation in the collected fraction. Biform complex was prepared by fusion method with a constant ratio of drug and cow ghee fraction. The prepared complex was subjected to FTIR, DSC, and LC-MS study to confirm chemical composition characteristics. Drug content, in-vitro and ex-vivo permeation studies were also performed. The anti-inflammatory response was measured using the carrageenan paw-induced edema rat model. Lipid-lowering effect and inflammation marker analysis was also performed using ELISA specific kit. \u0000\u0000\u0000\u0000\u0000The biform complex prepared with a thermal fraction at 30ºC of cow ghee show the highest in-vitro and ex-vivo permeation. The anti-inflammation response of the biform complex F1 was higher than other tested formulations with considerable lipid and lipoprotein lowering properties. \u0000\u0000\u0000\u0000\u0000 This study confirms that the thermal fractionation method abled to separate cow ghee as per their fatty acid content. The complexion of rosuvastatin calcium with cow ghee thermal fraction enhances oral bioavailability followed by the anti-inflammatory and lipid-lowering activity.\u0000\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45814457","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 : 2021-08-27DOI: 10.2174/2210303111666210827094543
Chaitali Taiwade, Aditi Fulfager, Hardik Bhargave, Govind Soni, K. Yadav
Erlotinib is a tyrosine kinase inhibitor and it can treat tumors, such as pancreatic and locally advanced lung cancer or metastatic cancer. The traditional formulation of erlotinib currently available is an oral delivery type that presents serious side effects such as hepatotoxicity, skin rashes, gastrointestinal disturbance, renal dysfunction, drug resistance and hematological symptoms. Besides this, other disadvantages of erlotinib provided mostly by oral administration are the comprehensive metabolism, low bioavailability, poor solubility and off-target impact. Overcoming such unfavorable attributes of the medication, innovative medication delivery mechanisms like nanocapsules, liposomes, microspheres, microparticles solid lipid nanoparticles, nanosponge, and nanoparticles have been studied that have really shown their lead over traditional formulations. This article summarizes the novel erlotinib drug delivery systems to boost its clinical efficacy and reduce systemic toxicity. Novel formulations of erlotinib will offer positive outcomes in cancer therapy and will play an important part in improving the drug's therapeutic potential.
{"title":"Erlotinib Hydrochloride Novel Drug Delivery Systems: A mini review unravelling the role of micro- and nanocarriers","authors":"Chaitali Taiwade, Aditi Fulfager, Hardik Bhargave, Govind Soni, K. Yadav","doi":"10.2174/2210303111666210827094543","DOIUrl":"https://doi.org/10.2174/2210303111666210827094543","url":null,"abstract":"\u0000\u0000Erlotinib is a tyrosine kinase inhibitor and it can treat tumors, such as pancreatic and locally advanced lung cancer or metastatic cancer. The traditional formulation of erlotinib currently available is an oral delivery type that presents serious side effects such as hepatotoxicity, skin rashes, gastrointestinal disturbance, renal dysfunction, drug resistance and hematological symptoms. Besides this, other disadvantages of erlotinib provided mostly by oral administration are the comprehensive metabolism, low bioavailability, poor solubility and off-target impact. Overcoming such unfavorable attributes of the medication, innovative medication delivery mechanisms like nanocapsules, liposomes, microspheres, microparticles solid lipid nanoparticles, nanosponge, and nanoparticles have been studied that have really shown their lead over traditional formulations. This article summarizes the novel erlotinib drug delivery systems to boost its clinical efficacy and reduce systemic toxicity. Novel formulations of erlotinib will offer positive outcomes in cancer therapy and will play an important part in improving the drug's therapeutic potential.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46748586","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 : 2021-08-12DOI: 10.2174/2210303111666210812160624
M. M. Priyanka, Shinde A. Ujwala, Sheth M. Kalyani, N. Desai
Acyclovir, BCS Class III drug is commercially available as 3 % w/w eye ointment for multiple applications. Acyclovir nanoemulsions can be proposed to reduce dose because of improved permeation characteristics. Further, the development of in situ ophthalmic gels can be advantageous to reduce the number of applications due to increased mucoadhesion and sustaining effect. The purpose of this study was the development and evaluation of nanoemulsions based in situ gels of Acyclovir (1% w/w) as potential ophthalmic delivery systems. Nanoemulsions of Acyclovir were developed by Phase Inversion Temperature method using Capmul MCM, stearyl amine and Kolliphor RH 40 as liquid lipid, charge inducer and surfactant, respectively selected on the basis of Acyclovir solubility studies in the oil phase and emulsification ability of surfactants. These nanoemulsions were further developed into in situ ophthalmic gels using gellan gum and Methocel K4M. The developed gels showed a sustained effect in vitro release studies and improved goat corneal permeation in ex vivo studies when compared to marketed ointment. HET-CAM studies concluded the absence of irritation potential, while in vivo irritation study in Wistar rats showed the absence of erythema and swelling of eyes after visual inspection for 72 hours. Histopathological studies on isolated rat corneas showed no abnormalities in anterior corneal epithelium and corneal stroma without any epithelial hyperplasia. Acyclovir nanoemulsions based in situ ophthalmic gel showed increased corneal deposition and permeation in rat eyes. The improved potential of developed ophthalmic gels was proven due to the reduced frequency of application compared to the marketed ointment in animal studies.
{"title":"In Situ Gels of Acylovir Nanoemulsions For Improved Delivery to The Eye","authors":"M. M. Priyanka, Shinde A. Ujwala, Sheth M. Kalyani, N. Desai","doi":"10.2174/2210303111666210812160624","DOIUrl":"https://doi.org/10.2174/2210303111666210812160624","url":null,"abstract":"\u0000\u0000Acyclovir, BCS Class III drug is commercially available as 3 % w/w eye ointment for multiple applications. Acyclovir nanoemulsions can be proposed to reduce dose because of improved permeation characteristics. Further, the development of in situ ophthalmic gels can be advantageous to reduce the number of applications due to increased mucoadhesion and sustaining effect. \u0000\u0000\u0000\u0000The purpose of this study was the development and evaluation of nanoemulsions based in situ gels of Acyclovir (1% w/w) as potential ophthalmic delivery systems. \u0000\u0000\u0000\u0000Nanoemulsions of Acyclovir were developed by Phase Inversion Temperature method using Capmul MCM, stearyl amine and Kolliphor RH 40 as liquid lipid, charge inducer and surfactant, respectively selected on the basis of Acyclovir solubility studies in the oil phase and emulsification ability of surfactants. These nanoemulsions were further developed into in situ ophthalmic gels using gellan gum and Methocel K4M. \u0000\u0000\u0000\u0000The developed gels showed a sustained effect in vitro release studies and improved goat corneal permeation in ex vivo studies when compared to marketed ointment. HET-CAM studies concluded the absence of irritation potential, while in vivo irritation study in Wistar rats showed the absence of erythema and swelling of eyes after visual inspection for 72 hours. Histopathological studies on isolated rat corneas showed no abnormalities in anterior corneal epithelium and corneal stroma without any epithelial hyperplasia. Acyclovir nanoemulsions based in situ ophthalmic gel showed increased corneal deposition and permeation in rat eyes. \u0000\u0000\u0000\u0000The improved potential of developed ophthalmic gels was proven due to the reduced frequency of application compared to the marketed ointment in animal studies.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-08-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47790581","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 : 2021-07-12DOI: 10.2174/2210303111666210712101322
Mohit Kumar, U. Mandal
The objective of the present article is to review various aspects of dissolution studies of dosage forms performed with the flow-through apparatus (USP type–IV apparatus). USP type-IV apparatus is comprised of a pump that compels the dissolution media upwards via the flow-through cell. A reservoir of dissolution medium is attached to the cell that is mounted vertically with a filter system to restrain the escape of un-dissolved particles. The apparatus is specially designed for powders, micro particles, pellets, and tablets. In this type of in vitro dissolution method, the test sample is placed in the bottom of the small-volume flow-through cell, and the solvent passes through it at a temperature of 37°C. This study is significant to build up the in-vivo and in-vitro relationship. Likewise, this study is used to distinguish the extent of medication released from the tested sample to foresee it’s in vivo viability in the actual patient population. The flow-through cell is used to determine the dissolution of micro-particulate, suppositories, implants, controlled-release formulations with drugs that have very low aqueous solubility. The drugs with small particle size and large surface area are dissolved at a faster rate as compared to other existing and compendia dissolution apparatuses. The article also highlights some of the in vitro dissolution studies carried out with the USP type-IV apparatus.
{"title":"In-vitro Dissolution Study of Pharmaceutical Products with USP Apparatus–IV","authors":"Mohit Kumar, U. Mandal","doi":"10.2174/2210303111666210712101322","DOIUrl":"https://doi.org/10.2174/2210303111666210712101322","url":null,"abstract":"\u0000\u0000The objective of the present article is to review various aspects of dissolution studies of dosage forms performed with the flow-through apparatus (USP type–IV apparatus). USP type-IV apparatus is comprised of a pump that compels the dissolution media upwards via the flow-through cell. A reservoir of dissolution medium is attached to the cell that is mounted vertically with a filter system to restrain the escape of un-dissolved particles. The apparatus is specially designed for powders, micro particles, pellets, and tablets. In this type of in vitro dissolution method, the test sample is placed in the bottom of the small-volume flow-through cell, and the solvent passes through it at a temperature of 37°C. This study is significant to build up the in-vivo and in-vitro relationship. Likewise, this study is used to distinguish the extent of medication released from the tested sample to foresee it’s in vivo viability in the actual patient population. The flow-through cell is used to determine the dissolution of micro-particulate, suppositories, implants, controlled-release formulations with drugs that have very low aqueous solubility. The drugs with small particle size and large surface area are dissolved at a faster rate as compared to other existing and compendia dissolution apparatuses. The article also highlights some of the in vitro dissolution studies carried out with the USP type-IV apparatus.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48895873","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 : 2021-07-12DOI: 10.2174/2210303111666210712100722
Devika Tripathi, Nandini Chaudhary, P. Wal, A. Rai, Jagannath Sahoo
Critically challenging tasks for the researchers are isolation and extraction of chief medicinally phytoconstituents from naturally existing herbal plants. The intricate process of extraction usually involves both plant and active animal portions medicinally separated and selective solvents through standard procedures. So, most of the products contain complex mixtures of metabolites; therefore, the extraction process cycle involved in separating these products makes it increasingly difficult and indicated yields in decimals. Thus, an alternative strategy suitable for green extraction routes has recently been obtained from sustainable resources with high solvency, low toxicity, and low environmental impacts, readily biodegradable, and recycled without detrimental effects on the environment. The process of the green hydrotrope-assisted extraction process persists in a novel and promising methodology. It maximizes the yield of phytoconstituents compared to the conventional extraction process by the employment of a variety of hydrotropes like sodium cumene sulfonate, sodium alkyl-benzene sulfonates, and sodium butyl mono-glycol sulfate. It is also involved in selective extraction of water-insoluble phytoconstituents by disorganization of the phospholipid bilayers and the aforementioned hydrotrope molecules through cell permeabilization, disrupting the cellulosic cell wall, then possibly the dissolution of the cellular contents. The central point of this audit is the increase of the surrender of phytoconstituents from herbal plants accomplished by the consideration of green hydrotropic-assisted extraction process, an assignment of dissolvable for the extraction of herbal grown plant, sanctioning of hydrotropes, its component, imperatively highlighting conveyance frameworks of separated extricated phytoconstituents from herbal plants to move forward their bioavailability at distinctive target destinations and its different utility angles have reflected effectively.
{"title":"Greenhydrotropes-assisted route an alternative approach for extracting phytoconstituents and associateddrug delivery systems","authors":"Devika Tripathi, Nandini Chaudhary, P. Wal, A. Rai, Jagannath Sahoo","doi":"10.2174/2210303111666210712100722","DOIUrl":"https://doi.org/10.2174/2210303111666210712100722","url":null,"abstract":"\u0000\u0000Critically challenging tasks for the researchers are isolation and extraction of chief medicinally phytoconstituents from naturally existing herbal plants. The intricate process of extraction usually involves both plant and active animal portions medicinally separated and selective solvents through standard procedures. So, most of the products contain complex mixtures of metabolites; therefore, the extraction process cycle involved in separating these products makes it increasingly difficult and indicated yields in decimals. Thus, an alternative strategy suitable for green extraction routes has recently been obtained from sustainable resources with high solvency, low toxicity, and low environmental impacts, readily biodegradable, and recycled without detrimental effects on the environment.\u0000\u0000\u0000\u0000\u0000The process of the green hydrotrope-assisted extraction process persists in a novel and promising methodology. It maximizes the yield of phytoconstituents compared to the conventional extraction process by the employment of a variety of hydrotropes like sodium cumene sulfonate, sodium alkyl-benzene sulfonates, and sodium butyl mono-glycol sulfate. It is also involved in selective extraction of water-insoluble phytoconstituents by disorganization of the phospholipid bilayers and the aforementioned hydrotrope molecules through cell permeabilization, disrupting the cellulosic cell wall, then possibly the dissolution of the cellular contents.\u0000\u0000\u0000\u0000\u0000The central point of this audit is the increase of the surrender of phytoconstituents from herbal plants accomplished by the consideration of green hydrotropic-assisted extraction process, an assignment of dissolvable for the extraction of herbal grown plant, sanctioning of hydrotropes, its component, imperatively highlighting conveyance frameworks of separated extricated phytoconstituents from herbal plants to move forward their bioavailability at distinctive target destinations and its different utility angles have reflected effectively.\u0000\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-07-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49460797","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 : 2021-06-16DOI: 10.2174/2210303111666210616115543
V. Agarwal, Nitin Kaushik, P. Sharma
This review paper gives focus on the nanocrystal approaches and their uses in pharmaceutical applications. Also, various preparation methods of the nanocrystal are briefly described in this presented review paper. The paper also describes several factors that are involved in the production of stable drug nanocrystals and provides suggestions for overcoming instability-related issues like aggregation and Ostwald ripening. Finally, the specific opportunities and challenges that are applicable to nanocrystal technology are summarized in this paper. In this paper, we summarize and discuss the special features of drug nanocrystals that include the enhancement of dissolution velocity, adhesiveness to the surface, and saturation solubility. Nowadays, pharmaceutical industries are using different approaches to prepare the nanocrystal, like bottom-up approach (precipitation), the top-down approach (wet milling, high-pressure homogenization), and some other combinational approaches. Drug nanocrystals can be administered through different routes. Besides this, the various fabrication methods and characterization methods may be used for the development and scale-up production of drug nanocrystals. In this review article, the relevance of drug nanocrystals are presented and illustrated according to their research done by different researchers and finally concluded that marketed formulation related to nanocrystal are gradually in progression. However, some related and developed formulations are under clinical trial. Poor solubility of the drug compounds is a major problem in the pharmaceutical field; therefore, the reduction of particle size may be one of the simplest and efficient processes for enhancing the solubility of such compounds. Drug nanocrystals are the crystals available with some drugs and having a particle size range of 100 to 1000 nm, covered by stabilization.
{"title":"Nanocrystal Approaches for Poorly Soluble Drugs and their Role in Development of Marketed Formulation","authors":"V. Agarwal, Nitin Kaushik, P. Sharma","doi":"10.2174/2210303111666210616115543","DOIUrl":"https://doi.org/10.2174/2210303111666210616115543","url":null,"abstract":"\u0000\u0000 This review paper gives focus on the nanocrystal approaches and their uses in pharmaceutical applications. Also, various preparation methods of the nanocrystal are briefly described in this presented review paper. The paper also describes several factors that are involved in the production of stable drug nanocrystals and provides suggestions for overcoming instability-related issues like aggregation and Ostwald ripening. Finally, the specific opportunities and challenges that are applicable to nanocrystal technology are summarized in this paper.\u0000\u0000\u0000\u0000In this paper, we summarize and discuss the special features of drug nanocrystals that include the enhancement of dissolution velocity, adhesiveness to the surface, and saturation solubility. Nowadays, pharmaceutical industries are using different approaches to prepare the nanocrystal, like bottom-up approach (precipitation), the top-down approach (wet milling, high-pressure homogenization), and some other combinational approaches. \u0000\u0000\u0000\u0000\u0000 Drug nanocrystals can be administered through different routes. Besides this, the various fabrication methods and characterization methods may be used for the development and scale-up production of drug nanocrystals.\u0000\u0000\u0000\u0000In this review article, the relevance of drug nanocrystals are presented and illustrated according to their research done by different researchers and finally concluded that marketed formulation related to nanocrystal are gradually in progression. However, some related and developed formulations are under clinical trial.\u0000\u0000\u0000\u0000Poor solubility of the drug compounds is a major problem in the pharmaceutical field; therefore, the reduction of particle size may be one of the simplest and efficient processes for enhancing the solubility of such compounds. Drug nanocrystals are the crystals available with some drugs and having a particle size range of 100 to 1000 nm, covered by stabilization.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48252938","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 : 2020-08-31DOI: 10.2174/2210303110666200206114632
S. B. Patil, Syed Z. Inamdar, K. R. Reddy, A. Raghu, K. G. Akamanchi, A. Inamadar, Kusal K. Das, R. V. Kulkarni
To develop electro-sensitive transdermal drug delivery systems (ETDDS) using polyacrylamide-grafted-pectin (PAAm-g-PCT) copolymer hydrogel for rivastigmine delivery. Free radical polymerization and alkaline hydrolysis technique was employed to synthesize PAAm-g-PCT copolymer hydrogel. The PAAm-g-PCT copolymeric hydrogel was used as a reservoir and cross-linked blend films of PCT and poly(vinyl alcohol) as rate-controlling membranes (RCMs) to prepare ETDDS. The pH of the hydrogel reservoir was found to be in the range of 6.81 to 6.93 and drug content was 89.05 to 96.29%. The thickness of RCMs was in the range of 51 to 99 μ and RCMs showed permeability behavior against water vapors. There was a reduction in the water vapor transmission rate as the glutaraldehyde (GA) concentration was increased. The drug permeation rate from the ETDDS was enhanced under the influence of electric stimulus against the absence of an electric stimulus. The increase in flux by 1.5 fold was recorded with applied electric stimulus. The reduction in drug permeability observed when the concentration of GA was increased. Whereas, the permeability of the drug was augmented as an electric current was changed from 2 to 8 mA. The pulsatile drug release under “on– off” cycle of electric stimulus witnessed a faster drug release under ‘on’ condition and it was slow under ‘off’ condition. The alteration in skin composition after electrical stimulation was confirmed through histopathology studies. The PAAm-g-PCT copolymer hydrogel is a useful carrier for transdermal drug delivery activated by an electric signal to provide on-demand release of rivastigmine.
{"title":"Functionally Tailored Electro-Sensitive Poly(Acrylamide)-g-Pectin Copolymer Hydrogel for Transdermal Drug Delivery Application: Synthesis, Characterization, In-vitro and Ex-vivo Evaluation","authors":"S. B. Patil, Syed Z. Inamdar, K. R. Reddy, A. Raghu, K. G. Akamanchi, A. Inamadar, Kusal K. Das, R. V. Kulkarni","doi":"10.2174/2210303110666200206114632","DOIUrl":"https://doi.org/10.2174/2210303110666200206114632","url":null,"abstract":"\u0000\u0000To develop electro-sensitive transdermal drug delivery systems (ETDDS) using\u0000polyacrylamide-grafted-pectin (PAAm-g-PCT) copolymer hydrogel for rivastigmine delivery.\u0000\u0000\u0000\u0000Free radical polymerization and alkaline hydrolysis technique was employed to synthesize\u0000PAAm-g-PCT copolymer hydrogel. The PAAm-g-PCT copolymeric hydrogel was used as a reservoir\u0000and cross-linked blend films of PCT and poly(vinyl alcohol) as rate-controlling membranes (RCMs) to\u0000prepare ETDDS.\u0000\u0000\u0000\u0000The pH of the hydrogel reservoir was found to be in the range of 6.81 to 6.93 and drug content\u0000was 89.05 to 96.29%. The thickness of RCMs was in the range of 51 to 99 μ and RCMs showed permeability\u0000behavior against water vapors. There was a reduction in the water vapor transmission rate as\u0000the glutaraldehyde (GA) concentration was increased. The drug permeation rate from the ETDDS was\u0000enhanced under the influence of electric stimulus against the absence of an electric stimulus. The increase\u0000in flux by 1.5 fold was recorded with applied electric stimulus. The reduction in drug permeability\u0000observed when the concentration of GA was increased. Whereas, the permeability of the drug was\u0000augmented as an electric current was changed from 2 to 8 mA. The pulsatile drug release under “on–\u0000off” cycle of electric stimulus witnessed a faster drug release under ‘on’ condition and it was slow under\u0000‘off’ condition. The alteration in skin composition after electrical stimulation was confirmed\u0000through histopathology studies.\u0000\u0000\u0000\u0000The PAAm-g-PCT copolymer hydrogel is a useful carrier for transdermal drug delivery\u0000activated by an electric signal to provide on-demand release of rivastigmine.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47041684","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 : 2020-08-31DOI: 10.2174/2210303109666190807104437
Giulia Anderluzzi, Y. Perrie
Solid lipid nanoparticles are lipid-based carriers that can be used for a range of drugs and biomolecules. However, most production methods currently used do not offer easy translation from laboratory preparation to scale-independent production. Within this study, we have investigated the use of microfluidics to produce solid lipid nanoparticles and investigated their protein loading capability. In the development of this process, we have investigated and identified the critical process parameters that impact on the product attributes of the solid lipid nanoparticles. Solid lipid nanoparticles based on Tristearin and 1,2-Distearoyl-phosphatidylethanolaminemethyl- polyethyleneglycol conjugate-2000 were formulated using the NanoAssemblr® Benchtop system. The flow rate ratio, total flow rate and initial protein concentration were investigated as process parameters and the particle size, PDI, zeta potential, drug loading and drug release were measured as product attributes. Our results demonstrate the suitability of microfluidics as a production method for solid lipid nanoparticles containing protein. In terms of key process parameters to consider, both the solvent to aqueous flow rate ratio and the total flow rate were shown to have a notable impact on particle size. Protein loading capacity was influenced by the solvent to aqueous flow rate ratio but was similar across all flow rates tested. Within this study, we outline a rapid and easy protocol for the scale-independent production of solid lipid nanoparticles. This process can support the rapid translation of production methods from bench to clinic.
{"title":"Microfluidic Manufacture of Solid Lipid Nanoparticles: A Case Study on Tristearin-Based Systems","authors":"Giulia Anderluzzi, Y. Perrie","doi":"10.2174/2210303109666190807104437","DOIUrl":"https://doi.org/10.2174/2210303109666190807104437","url":null,"abstract":"\u0000\u0000Solid lipid nanoparticles are lipid-based carriers that can be used for a range of\u0000drugs and biomolecules. However, most production methods currently used do not offer easy translation\u0000from laboratory preparation to scale-independent production.\u0000\u0000\u0000\u0000Within this study, we have investigated the use of microfluidics to produce solid lipid\u0000nanoparticles and investigated their protein loading capability. In the development of this process, we\u0000have investigated and identified the critical process parameters that impact on the product attributes of\u0000the solid lipid nanoparticles.\u0000\u0000\u0000\u0000Solid lipid nanoparticles based on Tristearin and 1,2-Distearoyl-phosphatidylethanolaminemethyl-\u0000polyethyleneglycol conjugate-2000 were formulated using the NanoAssemblr® Benchtop system.\u0000The flow rate ratio, total flow rate and initial protein concentration were investigated as process parameters\u0000and the particle size, PDI, zeta potential, drug loading and drug release were measured as\u0000product attributes.\u0000\u0000\u0000\u0000Our results demonstrate the suitability of microfluidics as a production method for solid lipid\u0000nanoparticles containing protein. In terms of key process parameters to consider, both the solvent to\u0000aqueous flow rate ratio and the total flow rate were shown to have a notable impact on particle size. Protein\u0000loading capacity was influenced by the solvent to aqueous flow rate ratio but was similar across all\u0000flow rates tested.\u0000\u0000\u0000\u0000Within this study, we outline a rapid and easy protocol for the scale-independent production\u0000of solid lipid nanoparticles. This process can support the rapid translation of production methods\u0000from bench to clinic.\u0000","PeriodicalId":11310,"journal":{"name":"Drug Delivery Letters","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46951719","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 : 2020-02-12DOI: 10.2174/2210303109666190717155731
H. Ranpise, K. Gujar, S. Pawar, R. Awasthi, K. Dua, D. Mathure, J. Madan
Ketoconazole is used in the treatment of superficial and systemic fungal infections. It acts by blocking the synthesis of ergosterol, an essential component of the fungal cell membrane. The purpose of this work was to formulate ketoconazole loaded nanostructured lipid carriers formulation for skin targeting to minimize the adverse side effects and to prolong release. The ketoconazole loaded nanostructured lipid carriers were optimized using 32 factorial design to evaluate the effects of process and formulation variables. The nanostructured lipid carriers were prepared by melt-dispersion ultra-sonication method. The formulations were finally incorporated into polymeric gels of Carbopol 940 for convenient application. The gels were evaluated comparatively with commercially available formulations of ketoconazole with respect to ex vivo skin permeation and deposition study on human cadaver skin. Nanostructured lipid carriers showed average particle size, zeta potential, and percentage entrapment in the range of 125.8 ± 1.8 to 295.0 ± 3.8 nm, -13.2 ± 1.1 to -30.9 ± 2.2 mV, and 69.47 ± 2.8 to 95.49 ± 4.5, respectively. Thermal studies revealed no drug-excipient incompatibility and amorphization of ketoconazole. Ex vivo study of the gel exhibited prolonged drug release up to 12 h. In vitro drug deposition study showed that the gel formulation can avoid the systemic uptake, better accumulative uptake of the drug, and nonirritant to the skin compared to marketed formulation. Optimized formulation exhibited better antifungal activity when compared to ketoconazole loaded gel and marketed cream (Keto ® cream). Histolopathology results indicated no toxic effect on the skin. These results indicate that developed nanostructured lipid-carriers gel formulation represents a promising carrier for topical delivery of ketoconazole, having controlled drug release, and potential of skin targeting.
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