Department of Chemistry, Sunandan Divatia School of science, SVKM's NMIMS (Deemed-to-be) University, Vile Parle-West, Mumbai, 400056, Maharashtra, India.
J Pharm Biomed Anal. 2019 Apr 15;167:66-73. doi: 10.1016/j.jpba.2018.12.018. Epub 2019 Feb 1.
Acetyl- Keto-β-boswellic acid (AKBA) is a pentacyclic triterpenic acid found in gum resin of Boswellia serrata. Even though it is shown to have anti-inflammatory activity, its bioavailability gets limited due to its poor aqueous solubility and permeability. The present study, hence, deals in enhancement of the intestinal absorption of AKBA from total boswellic acid fraction (TA fraction) using cyclodextrin (CD) and poloxamer solid dispersion (PXM SDs) formulations. Absorption studies were performed using the everted gut sac model prepared from rat jejunum. The glucose uptake assay was performed to show viability of gut sac tissue. The apparent permeability (P) value of AKBA from TA fraction was 1.08 ± 0.17 × 10 which was found to be increased by 10-14 fold with CD complex and SD formulations. The intestinal absorption studies showed highest absorption of AKBA from HP-β-CD complex and PXM 407 SD as compared to that from TA fraction. From this study, it can be concluded that HP-β-CD and PXM 407 effectively enhanced intestinal absorption through improved solubility, highlighting their role as efficient drug delivery agents and bioavailability enhancers.
乙酰-酮-β-乳香酸（AKBA）是一种五环三萜酸，存在于乳香树的胶树脂中。尽管它具有抗炎活性，但由于其较差的水溶性和渗透性，其生物利用度受到限制。因此，本研究旨在通过环糊精（CD）和泊洛沙姆固体分散体（PXM SDs）制剂来提高总乳香酸（TA）部分中的 AKBA 的肠道吸收。采用大鼠空肠制备的外翻肠囊模型进行吸收研究。葡萄糖摄取试验用于显示肠囊组织的活力。TA 部分中 AKBA 的表观渗透（P）值为 1.08 ± 0.17×10，用 CD 配合物和 SD 制剂处理后，发现其增加了 10-14 倍。肠道吸收研究表明，与 TA 部分相比，HP-β-CD 配合物和 PXM 407 SD 中 AKBA 的吸收最高。从这项研究可以得出结论，HP-β-CD 和 PXM 407 通过提高溶解度有效地增强了肠道吸收，突出了它们作为有效药物递送剂和生物利用度增强剂的作用。
