QbD-guided phospholipid-tagged nanonized boswellic acid naturosomal delivery for effective rheumatoid arthritis treatment

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics: X Pub Date : 2024-05-19 DOI:10.1016/j.ijpx.2024.100257
Poonam Usapkar , Suprit Saoji , Pradnya Jagtap , Muniappan Ayyanar , Mohan Kalaskar , Nilambari Gurav , Sameer Nadaf , Satyendra Prasad , Damiki Laloo , Mohd Shahnawaz Khan , Rupesh Chikhale , Shailendra Gurav
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Abstract

Studies have reported the potential role of Boswellic acids (BAs), bioactive pentacyclic triterpenes from Boswellia serrata (BS), in treating rheumatoid arthritis (RA). However, poor water solubility and limited oral absorption are restricting factors for its better therapeutic efficacy. Based on these assumptions, the current study aimed to develop naturosomal delivery of BAs to boost their extremely low bioavailability, colloidal stability, and water solubility. Nanonized naturosomes were developed and subsequently analyzed to show their physicochemical and functional features employing the quality-by-design approach. The solubility analysis of Boswellic acid naturosomes revealed a 16 times improvement in aqueous solubility compared to BS extract (BSE). The zeta potential and dynamic light scattering findings of BSE naturosomes (BSENs) have demonstrated their colloidal stability with regulated nano-size particles. Additionally, compared to BSE (⁓31%), in-vitro dissolution experiments showed that >99% of pentacyclic triterpenes were released from BSENs. Studies on ex-vivo permeation showed that BSENs' permeation (>79%) significantly improved over BSE's (⁓20%). In-vivo efficacy studies using CFA-prompted arthritis in rodents showed a critical expansion in body wt and an undeniable reduction in paw thickness, paw volume, and TNF-α treated with BSEN compared to the arthritis control and BSE-treated group. These findings suggest that BSENs can help treat RA drugs by demonstrating their efficacy in further clinical research to validate the significant improvements.

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QbD 引导下的磷脂标记纳米化乳香酸纳豆体递送技术用于类风湿性关节炎的有效治疗
有研究报告称,乳香酸(BAs)--来自乳香(BS)的具有生物活性的五环三萜--在治疗类风湿性关节炎(RA)方面具有潜在作用。然而,水溶性差和口服吸收受限是限制其发挥更好疗效的因素。基于这些假设,目前的研究旨在开发天然神经体输送 BA,以提高其极低的生物利用度、胶体稳定性和水溶性。研究人员开发了纳米化的纳豆体,随后采用质量源于设计的方法对其进行了分析,以显示其理化和功能特征。乳香酸纳豆体的溶解度分析表明,其水溶性比 BS 提取物(BSE)提高了 16 倍。乳香酸纳豆体(BSENs)的ZETA电位和动态光散射研究结果表明,其具有调节纳米尺寸颗粒的胶体稳定性。此外,与 BSE(⁓31%)相比,体外溶解实验表明 BSENs 释放了 99% 的五环三萜。体内外渗透性研究表明,BSENs 的渗透性(>79%)比 BSE 的渗透性(⁓20%)显著提高。使用 CFA 诱导的啮齿动物关节炎进行的体内疗效研究表明,与关节炎对照组和 BSE 治疗组相比,BSEN 治疗组的体重明显增加,爪厚、爪体积和 TNF-α 均明显减少。这些研究结果表明,BSEN 可以帮助治疗 RA 药物,通过进一步的临床研究来验证其疗效,从而验证其显著的改善作用。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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