Pichayakorn Wiwat, Monton Chaowalit, Sampaopan Yupaporn, Panrat Kamon, Suksaeree Jirapornchai
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, 90112, Thailand.
Drug and Herbal Product Research and Development Center, College of Pharmacy, Rangsit University, Muang, Pathum Thani, 12000, Thailand.
AAPS PharmSciTech. 2022 Jul 12;23(6):194. doi: 10.1208/s12249-022-02341-6.
Lysiphyllum strychnifolium has long been used as a popular herbal medicinal plant for treating fever and alcohol intoxication. This study aimed to prepare buccal film for L. strychnifolium stem extracts. These extracts were less soluble in water and were therefore loaded in self-emulsifying systems before being mixed into the film. Astilbin was selected as a chemical marker in L. strychnifolium stem extracts. Firstly, the L. strychnifolium stem extracts were entrapped in the self-emulsifying systems which were designed and optimized based on 3 factorial design. The optimal formulation was 0.60 g of surfactant-co-surfactant mixture (Tween 80 and polyethylene glycol 400 in the ratio of 7.5:1) and 0.40 g of caprylic/capric triglyceride. Secondly, the optimal self-emulsifying system was loaded in the polymeric film which consisted of polyvinyl alcohol blended with poloxamer 407 using glycerin as a plasticizer. The properties of the prepared buccal film were unchanged, and the film showed an amorphous state, indicating all ingredients might be completely dissolved in the film. The buccal film could be placed in direct contact with the mouth without oral mucosal irritation, and showed a smooth and homogeneous surface with a rough and compact cross-sectional morphology. Astilbin content in the buccal film was 61.39 ± 11.45 µg/cm. Astilbin was released from the buccal film while the permeation rate was low. The release mechanism was both swelling and diffusion, and followed anomalous or non-Fickian transfer. The permeability coefficient of the cumulative amount of astilbin permeated from buccal film was 1.0192 ± 0.1395 ×10 cm/h. Thus, the buccal film can be prepared by using a self-emulsifying system for herbal applications and shows potential as a safe and convenient form of oral drug administration.
马钱叶崖爬藤长期以来一直被用作治疗发热和酒精中毒的常用草药。本研究旨在制备马钱叶崖爬藤茎提取物口腔膜。这些提取物在水中的溶解度较低，因此在混入膜中之前先负载于自乳化系统中。选择二氢杨梅素作为马钱叶崖爬藤茎提取物中的化学标志物。首先，将马钱叶崖爬藤茎提取物包裹在基于三因素设计的自乳化系统中，该系统经过设计和优化。最佳配方为0.60 g表面活性剂-助表面活性剂混合物（吐温80和聚乙二醇400，比例为7.5:1）和0.40 g辛酸/癸酸甘油三酯。其次，将最佳自乳化系统负载于由聚乙烯醇与泊洛沙姆407共混并以甘油作为增塑剂组成的聚合物膜中。所制备口腔膜的性质未发生变化，且膜呈现非晶态，表明所有成分可能完全溶解于膜中。该口腔膜可直接与口腔接触而无口腔黏膜刺激性，表面光滑均匀，横截面形态粗糙致密。口腔膜中二氢杨梅素含量为61.39±11.45 μg/cm。二氢杨梅素从口腔膜中释放，但渗透速率较低。释放机制为溶胀和扩散，遵循非正规或非菲克扩散。二氢杨梅素从口腔膜中渗透的累积量的渗透系数为1.0192±0.1395×10 cm/h。因此，可通过自乳化系统制备用于草药应用的口腔膜，其作为一种安全便捷的口服给药形式具有潜力。
