Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria.
AIDS Res Ther. 2013 May 31;10(1):14. doi: 10.1186/1742-6405-10-14.
CSIC (5-chloro-3-phenylsulfonylindole-2-carboxamide), a non-nucleoside reverse transcriptase inhibitor (NNRTI) has not been advanced as a therapeutic anti-HIV candidate drug due to its low aqueous solubility and poor bioavailability.
The objective of this work was to formulate CSIC into self-emulsifying oil formulations for the purpose of improving its aqueous solubility and evaluating in vitro antiretroviral activity.
CSIC self-emulsifying oil formulations (SEFs) were formulated and evaluated for droplet size, zeta potential, polydispersity index (PDI), viscosity, emulsification time, stability and bioactivity.
Results showed significantly improved solubility of CSIC in the SEFs.The concentration of co-surfactant affected the droplet size, zeta potential and polydispersity index. In vitro bioactivity studies showed that the CSIC SEFs retained full anti-HIV activity.
The in vitro data from this first attempt to formulate CSIC SEFs suggest that improvement on the aqueous solubility of CSIC through this delivery system may accentuate its antiretroviral effectiveness in vivo via bioavailability enhancement. The formulation is therefore intended as an oral anti-HIV agent for prophylactic and therapeutic uses.
CSIC（5-氯-3-苯磺酰基吲哚-2-甲酰胺），一种非核苷类逆转录酶抑制剂（NNRTI），由于其低水溶性和差的生物利用度，尚未被作为治疗抗 HIV 的候选药物。
本工作的目的是将 CSIC 制成自乳化油制剂，以提高其水溶性，并评价其体外抗逆转录病毒活性。
对 CSIC 自乳化油制剂（SEFs）进行了制剂设计和评价，包括粒径、zeta 电位、多分散指数（PDI）、粘度、乳化时间、稳定性和生物活性。
结果表明 CSIC 在 SEFs 中的溶解度显著提高。助表面活性剂的浓度影响液滴大小、zeta 电位和多分散指数。体外生物活性研究表明 CSIC SEFs 保留了完整的抗 HIV 活性。
这是首次尝试将 CSIC SEFs 进行制剂设计，通过该传递系统提高 CSIC 的水溶性，可能通过提高生物利用度来增强其体内抗逆转录病毒效果。因此，该制剂旨在作为一种口服抗 HIV 药物，用于预防和治疗用途。
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