{"title":"Box-Behnken设计制备坎地沙坦固体脂质纳米颗粒","authors":"Yelugudhari Ramulu, D. Bhikshapathi","doi":"10.25004/ijpsdr.2021.130604","DOIUrl":null,"url":null,"abstract":"The primary motive behind this the present investigation was to develop and optimize the solid lipid nanoparticles formulation of candesartan to enhance solubility and dissolution rate. The prepared SLNs composed of precirol, poloxamer 188, soy lecithin, tween 80, were fabricated employing hot emulsification/ ultrasonication technique. Box-Behnken design was employed for 17 formulation batches in which 3 factors namely lipid, surfactant, and co-surfactant (precirol, poloxamer 188 and soy lecithin) tween 80 weretested at 3 levels of their concentration, i.e., low, medium and high. The effect of different levels of factors\nwas evaluated for the particle size, entrapment efficiency and % cumulative drug release. Kinetic model\nfitting for candesartan solid lipid nanoparticles (SLN) formulation was done to interpret the release rate\nfrom the SLN. Optimized formulation was subjected for fourier transform infrared spectroscopy (FTIR),\nscanning electron microscope (SEM) and stability studies. The mean particle size, PDI, zeta potential,\nentrapment efficiency, content uniformity and in-vitro drug release of optimized candesartan-loaded SLNs\n(CD10) were found to be 135.38 ± 3.41 nm, 0.125 ± 0.04, -18.16 ± 2.89 mV, 86.4 ± 2.35%, 99.78 ± 2.54%\nand 98.91 ± 0.85% respectively. The release kinetics suggested that drug release followed zero-order and\nrelease was anomalous non-fickian diffusion super case II transport. FTIR studies revealed no incompatibility\nbetween drug and excipients, SEM images exhibited nanoparticles to be more porous and in a spherical\nshape. Stability studies indicated good stability of the formulation. The proposed way of SLN preparation\ncould be considered a proper method for producing a candesartan-loaded colloidal carrier system.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"276 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development of Candesartan Loaded Solid Lipid Nanoparticles by Box-Behnken Design\",\"authors\":\"Yelugudhari Ramulu, D. Bhikshapathi\",\"doi\":\"10.25004/ijpsdr.2021.130604\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The primary motive behind this the present investigation was to develop and optimize the solid lipid nanoparticles formulation of candesartan to enhance solubility and dissolution rate. The prepared SLNs composed of precirol, poloxamer 188, soy lecithin, tween 80, were fabricated employing hot emulsification/ ultrasonication technique. Box-Behnken design was employed for 17 formulation batches in which 3 factors namely lipid, surfactant, and co-surfactant (precirol, poloxamer 188 and soy lecithin) tween 80 weretested at 3 levels of their concentration, i.e., low, medium and high. The effect of different levels of factors\\nwas evaluated for the particle size, entrapment efficiency and % cumulative drug release. Kinetic model\\nfitting for candesartan solid lipid nanoparticles (SLN) formulation was done to interpret the release rate\\nfrom the SLN. Optimized formulation was subjected for fourier transform infrared spectroscopy (FTIR),\\nscanning electron microscope (SEM) and stability studies. The mean particle size, PDI, zeta potential,\\nentrapment efficiency, content uniformity and in-vitro drug release of optimized candesartan-loaded SLNs\\n(CD10) were found to be 135.38 ± 3.41 nm, 0.125 ± 0.04, -18.16 ± 2.89 mV, 86.4 ± 2.35%, 99.78 ± 2.54%\\nand 98.91 ± 0.85% respectively. The release kinetics suggested that drug release followed zero-order and\\nrelease was anomalous non-fickian diffusion super case II transport. FTIR studies revealed no incompatibility\\nbetween drug and excipients, SEM images exhibited nanoparticles to be more porous and in a spherical\\nshape. Stability studies indicated good stability of the formulation. The proposed way of SLN preparation\\ncould be considered a proper method for producing a candesartan-loaded colloidal carrier system.\",\"PeriodicalId\":14278,\"journal\":{\"name\":\"International Journal of Pharmaceutical Sciences and Drug Research\",\"volume\":\"276 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-11-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Pharmaceutical Sciences and Drug Research\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.25004/ijpsdr.2021.130604\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Pharmaceutical Sciences and Drug Research","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25004/ijpsdr.2021.130604","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Development of Candesartan Loaded Solid Lipid Nanoparticles by Box-Behnken Design
The primary motive behind this the present investigation was to develop and optimize the solid lipid nanoparticles formulation of candesartan to enhance solubility and dissolution rate. The prepared SLNs composed of precirol, poloxamer 188, soy lecithin, tween 80, were fabricated employing hot emulsification/ ultrasonication technique. Box-Behnken design was employed for 17 formulation batches in which 3 factors namely lipid, surfactant, and co-surfactant (precirol, poloxamer 188 and soy lecithin) tween 80 weretested at 3 levels of their concentration, i.e., low, medium and high. The effect of different levels of factors
was evaluated for the particle size, entrapment efficiency and % cumulative drug release. Kinetic model
fitting for candesartan solid lipid nanoparticles (SLN) formulation was done to interpret the release rate
from the SLN. Optimized formulation was subjected for fourier transform infrared spectroscopy (FTIR),
scanning electron microscope (SEM) and stability studies. The mean particle size, PDI, zeta potential,
entrapment efficiency, content uniformity and in-vitro drug release of optimized candesartan-loaded SLNs
(CD10) were found to be 135.38 ± 3.41 nm, 0.125 ± 0.04, -18.16 ± 2.89 mV, 86.4 ± 2.35%, 99.78 ± 2.54%
and 98.91 ± 0.85% respectively. The release kinetics suggested that drug release followed zero-order and
release was anomalous non-fickian diffusion super case II transport. FTIR studies revealed no incompatibility
between drug and excipients, SEM images exhibited nanoparticles to be more porous and in a spherical
shape. Stability studies indicated good stability of the formulation. The proposed way of SLN preparation
could be considered a proper method for producing a candesartan-loaded colloidal carrier system.