Formulation and Evaluation of Solid Self Nano Emulsifying drug delivery System of Olanzapine to Enhance Aqueous Solubility and Dissolution Rate

M. Reddy, Baskarla Sravani
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引用次数: 2

Abstract

Present research work was aimed to enhance aqueous solubility and dissolution rate of olanzapine by solid self nano emulsifying drug delivery system(S-SNEDDS). Olanzapine is a BCS class II drug having 65% oral bioavailability; it is used in the treatment of psychosis, depression and mania conditions. Oils, Surfactants, Co surfactants were selected depending upon the saturated solubility of olanzapine in those components; excipients were screened depending on olanzapine solubility in various oils, surfactants and co surfactants. Surfactant: co surfactant {Smix} ratios i.e., 3:1 and 4:1 were prepared to determine nano emulsion regions and also to formulate liquid self nano emulsifying drug delivery system (L-SNEDDS). Pseudo ternary phase diagram were plotted by using Triplot version 4.1.2 software, nano emulsion region was determined and evaluated. Formulations were designed based on saturated solubility of olanzapine and Pseudo ternary phase diagram using various ratios of oils [Capryol 90], surfactants [Kolliphor EL], co surfactants [Lauroglycol 90] depending on its solubility and nano emulsion formation four formulations were developed which are further selected for characterisation of L-SNEDDS like robustness to dilution, self emulsification, determination of droplet size, PDI, Drug loading efficacy, zeta potential and also Invitro drug release. Among those four formulations, F1 (SB184J 4:6) was optimum because compared to other three formulations F3 gave best results in terms of droplet size (66nm) with PDI (0.24), Invitro drug release, dissolution rate of F1 SNEDDS having (88.201± 0.25%). Invitro drug release of F1 formulation was compared with that of Olanzapine [API] (45.281± 0.52%) the results indicating that there is a increase in solubility and dissolution rate of olanzapine by 2.2 times more compared to pure olanzapine (API). F1 (SB184J 4:6) were converted into S-SNEDDS by adsorption process by addition porous carriers (Aerosil 200). Formulated S-SNEDDS were undergone various evaluation parameters and also reconstitution parameters to determine Droplet size and Invitro drug release of solid F1 (SB184J4:6) formulation. The results of present study demonstrates that olanzapine SNEDDS has an ability and potential to enhance solubility and dissolution rate.
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提高奥氮平溶解度和溶出率的固体自纳米乳化给药体系的研制与评价
本研究旨在利用固体自纳米乳化给药系统(S-SNEDDS)提高奥氮平的水溶性和溶出率。奥氮平是BCS II类药物,具有65%的口服生物利用度;它用于治疗精神病、抑郁症和躁狂症。根据奥氮平在这些成分中的饱和溶解度来选择油、表面活性剂、钴表面活性剂;根据奥氮平在各种油脂、表面活性剂和辅助表面活性剂中的溶解度筛选辅料。表面活性剂:表面活性剂{Smix}的比例分别为3:1和4:1,以确定纳米乳区域,并制备液体自纳米乳化给药系统(L-SNEDDS)。采用Triplot 4.1.2版软件绘制伪三元相图,确定并评价纳米乳区。根据奥氮平的饱和溶解度和伪三元相图设计配方,使用不同比例的油[Capryol 90]、表面活性剂[Kolliphor EL]、辅表面活性剂[lauro乙二醇90],根据其溶解度和纳米乳液形成情况,开发了四种配方,并进一步选择用于L-SNEDDS的特性,如稀释稳健性、自乳化性、液滴大小、PDI、载药效率、zeta电位和体外药物释放。其中F1 (SB184J 4:6)为最佳配方,F3在微滴尺寸(66nm)、PDI(0.24)、体外释药、F1 SNEDDS溶出度(88.201±0.25%)方面均优于其他3个配方。F1制剂与奥氮平(API)体外释放量(45.281±0.52%)比较,结果表明,与纯奥氮平(API)相比,F1制剂的溶解度和溶出率提高了2.2倍。通过添加多孔载体(Aerosil 200),将F1 (SB184J 4:6)转化为S-SNEDDS。采用各种评价参数和重构参数测定固体F1 (SB184J4:6)制剂的滴度和体外药物释放度。本研究结果表明,奥氮平sndds具有提高溶解度和溶出率的能力和潜力。
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