Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu
{"title":"酮洛芬经皮给药纳米结构脂质载体的开发与评价","authors":"Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu","doi":"10.55262/fabadeczacilik.1126288","DOIUrl":null,"url":null,"abstract":"Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen. \nMethods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied. \nResults: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility. \nConclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.","PeriodicalId":36004,"journal":{"name":"Fabad Journal of Pharmaceutical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2022-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development and Evaluation of Nanostructured Lipid Carriers for Transdermal Delivery of Ketoprofen\",\"authors\":\"Thulasi Sathyanarayana, P. Sudheer, E. Jacob, Merlin Mary Sabu\",\"doi\":\"10.55262/fabadeczacilik.1126288\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen. \\nMethods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied. \\nResults: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility. \\nConclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.\",\"PeriodicalId\":36004,\"journal\":{\"name\":\"Fabad Journal of Pharmaceutical Sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-12-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Fabad Journal of Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.55262/fabadeczacilik.1126288\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Fabad Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.55262/fabadeczacilik.1126288","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Development and Evaluation of Nanostructured Lipid Carriers for Transdermal Delivery of Ketoprofen
Purpose: Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) which when administered via an oral route displays significant gastro-intestinal side effects and has low skin permeation profile. The objective of the present work is to utilise nanostructured lipid carriers (NLCs) as carrier system for transdermal delivery of ketoprofen.
Methods: NLCs were prepared via hot homogenisation technique using bees wax, carnauba wax, glycerl monostearate (solid lipids), linseed oil (liquid lipid) and poloxamer188 (surfactant) and optimized using custom design via JMP. The responses evaluated were drug entrapment efficiency, particle size and drug release profile. The experimental design was evaluated for model fit with the assistance of ANOVA. The optimum formulations were characterized for particle size, zeta potential, SEM, DSC, FTIR and also drug content, entrapment efficiency, in- vitro drug release, ex-vivo drug release profile was studied.
Results: The drug entrapment in the range of 34±0.03-95.06±0.01%. The drug release from the formulations over a 24 h study was found to be 80%±0.09 to 95%±0.06. The maximum desirability was found to be 0.91. The optimum formulation showed mean particle size of 425.8nm and a zeta potential of -45mV. SEM results revealed slightly agglomerated particles with uneven surfaces. The ex-vivo skin permeation of NLC optimized patch formulation exhibited a higher flux and permeability coefficient in comparison to the pure drug patch formulation and marketed gel (2.5%w/w) FTIR spectra assured the chemical and physical compatibility.
Conclusion: Transdermal delivery of ketoprofen via NLCs would be a promising approach for improving the skin permeation.
期刊介绍:
The FABAD Journal of Pharmaceutical Sciences is published triannually by the Society of Pharmaceutical Sciences of Ankara (FABAD). All expressions of opinion and statements of supposed facts appearing in articles and/or advertisiments carried in this journal are published on the responsibility of the author and/or advertiser, anda re not to be regarded those of the Society of Pharmaceutical Sciences of Ankara. The manuscript submitted to the Journal has the requirement of not being published previously and has not been submitted elsewhere. Manuscripts should be prepared in accordance with the requirements specified as given in detail in the section of “Information for Authors”. The submission of the manuscript to the Journal is not a condition for acceptance; articles are accepted or rejected on merit alone. All rights reserved.