Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo, Egypt.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo, Egypt.
Drug Des Devel Ther. 2022 Nov 4;16:3847-3864. doi: 10.2147/DDDT.S383051. eCollection 2022.
The objective of the present study was to scrutinize the microsponges (MS) as a carrier system using Adapalene (ADA) as a model drug.
Data modelling was implemented using Plackett-Burman design to identify the main variables affecting the formulation of ADA-MS. The adopted method of preparation for MS was quasi-emulsion solvent diffusion method. The nominated independent variables were volume of organic phase, sonication time, stirring speed, drug percent, polymer type, emulsifier concentration, and method of organic phase addition. As for the dependent variables, they included entrapment efficiency (E.E.%), production yield (P.Y.%), particle size (P.S.) and morphology. Furthermore, selected ADA loaded microsponges (ADA-MS) were in vitro assayed for their biological activities via cytotoxicity, UVA irradiation and cell viability, and antimicrobial activity.
The study indicated that the drug percent, polymer type and surfactant concentration have the key significant effect on E.E.% and P.Y.%, while, the drug percent, stirring speed and volume of organic phase have had a significant effect on P.S. and their morphology. Furthermore, ADA-MS had a momentous cytotoxic effect on A431 and M10 cell-lines with exceptional enrichment when the polymer Eudragit RS100 was used. Also, the ADA-MS increased the cell viability after UVA irradiation on HFB-4 cell-line by 14% to 43%, especially when using Ethyl Cellulose as a polymer. Lastly, the antimicrobial activity of ADA against was boosted when incorporated into MS.
The Plackett-Burman design proved its impact in discerning preparation variables affecting the quality of ADA-MS formulation, with heightening of the in vitro biological activities of ADA. Thus, MS was presumed to be an auspicious carrier system for ADA.
本研究的目的是研究微球（MS）作为一种载体系统，以阿达帕林（ADA）为模型药物。
采用 Plackett-Burman 设计对影响 ADA-MS 制剂的主要变量进行数据建模。采用准乳液溶剂扩散法制备 MS。选择的独立变量为有机相体积、超声时间、搅拌速度、药物百分比、聚合物类型、乳化剂浓度和有机相添加方式。对于因变量，它们包括包封效率（E.E.%）、产率（P.Y.）、粒径（P.S.）和形态。此外，通过细胞毒性、UVA 照射和细胞活力以及抗菌活性对选定的载有 ADA 的微球（ADA-MS）进行体外测定。
研究表明，药物百分比、聚合物类型和表面活性剂浓度对 E.E.%和 P.Y.有显著影响，而药物百分比、搅拌速度和有机相体积对 P.S.及其形态有显著影响。此外，ADA-MS 对 A431 和 M10 细胞系具有重要的细胞毒性作用，当使用 Eudragit RS100 聚合物时，其富集作用尤为明显。此外，ADA-MS 可将 HFB-4 细胞系经 UVA 照射后的细胞活力提高 14%至 43%，特别是当使用乙基纤维素作为聚合物时。最后，将 ADA 纳入 MS 可增强其对 的抗菌活性。
Plackett-Burman 设计证明了其在识别影响 ADA-MS 制剂质量的制备变量方面的作用，同时提高了 ADA 的体外生物活性。因此，MS 被认为是 ADA 的一种有前途的载体系统。
