Moussa Yomna A, Teaima Mahmoud H, Attia Dalia, Elmazar Mohey M, El-Nabarawi Mohamed A
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, The British University in Egypt (BUE), 11837 El-Sherouk City, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, 11562 Cairo, Egypt.
ACS Omega. 2023 Jun 1;8(23):20251-20261. doi: 10.1021/acsomega.2c06629. eCollection 2023 Jun 13.
Green coffee bean extract (GCBE) provides diversified health benefits. However, its reported low bioavailability impeded its utilization in various applications. In this study, GCBE-loaded solid lipid nanoparticles (SLNs) were prepared to improve the bioavailability through enhanced intestinal absorption of GCBE. During the preparation of promising GCBE-loaded SLNs, the lipid concentration, surfactant concentration, and co-surfactant amount are crucial that were optimized using the Box-Behnken design, while particle size, polydispersity index (PDI), ζ-potential, entrapment efficiency, and cumulative drug release were the measured responses. GCBE-SLNs were successfully developed by a high shear homogenization technique using geleol as a solid lipid, tween 80 as a surfactant, and propylene glycol as Co-SAA. The optimized SLNs contained 5.8% geleol, 5.9% tween 80, and 80.4 mg PG resulting in a small particle size of 235.7 ± 12.5 nm, reasonably acceptable PDI of 0.417 ± 0.023, and ζ-potential of -15 ± 0.14 mV, with a high entrapment efficiency of 58.3 ± 0.85% and cumulative release of 7575 ± 0.78%. Furthermore, the performance of the optimized GCBE-SLN was evaluated using an ex vivo everted sac model where the intestinal permeation of GCBE was improved due to nanoencapsulation using SLN. Consequently, the results enlightened the auspicious potential of exploiting oral GCBE-SLNs for boosting intestinal absorption of chlorogenic acid.
绿咖啡豆提取物（GCBE）具有多种健康益处。然而，据报道其生物利用度较低，这阻碍了它在各种应用中的使用。在本研究中，制备了负载GCBE的固体脂质纳米粒（SLN），以通过增强GCBE的肠道吸收来提高其生物利用度。在制备有前景的负载GCBE的SLN过程中，脂质浓度、表面活性剂浓度和助表面活性剂用量至关重要，使用Box-Behnken设计对其进行了优化，而粒径、多分散指数（PDI）、ζ电位、包封率和药物累积释放是测量的响应指标。采用高剪切均质技术，以凝胶醇为固体脂质、吐温80为表面活性剂、丙二醇为助表面活性剂，成功制备了GCBE-SLN。优化后的SLN含有5.8%的凝胶醇、5.9%的吐温80和80.4 mg丙二醇，粒径小，为235.7±12.5 nm，PDI合理，为0.417±0.023，ζ电位为-15±0.14 mV，包封率高，为5,8.3±0.85%，累积释放率为75.75±0.78%。此外，使用离体外翻肠囊模型评估了优化后的GCBE-SLN的性能，结果表明，由于使用SLN进行纳米包封，GCBE的肠道渗透得到了改善。因此，这些结果揭示了开发口服GCBE-SLN以促进绿原酸肠道吸收的良好潜力。
