使用辣木籽油负载他克莫司的纳米结构脂质载体：设计、优化和体外评价。

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2023-11-01 Epub Date: 2023-07-05 DOI:10.1080/02652048.2023.2231075

Rajat Garg, Anuj Garg

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引用次数: 0

摘要

拟议的研究旨在开发他克莫司负载的纳米结构脂质载体（TAC负载的NLCs），以克服较差的水溶性和溶解速率，增强其口服吸收。采用中心复合设计优化泊洛沙姆188和D-α-生育酚聚乙二醇琥珀酸酯（TPGS）的用量。优化的TAC负载NLC含有硬脂酸（250 mg）、辣木（MO）籽油（50 mg），TAC（他克莫司：10 mg），TPGS（60 mg）和平均直径为393.3的泊洛沙姆188（1%w/v） ± 29.68 nm，ζ电位为-18.3 ± 6.19 mV，截留效率高（92.12 ± 1.14%w/w）和可取性（0.989）。TAC负载的NLCs显示出约12倍的药物溶解效率，而体外抗炎研究显示IC50（最大抑制浓度的一半）比TAC悬浮液低约1.8倍。冻干的TAC负载的NLCs在3 月。因此，本研究得出结论，TAC在由硬脂酸和MO籽油制成的NLCs中的成功封装。

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Tacrolimus loaded nanostructured lipid carriers using Moringa oleifera seed oil: design, optimization and in-vitro evaluations.

The proposed research aims to develop Tacrolimus-loaded nanostructured lipid carriers (TAC-loaded NLCs) to overcome poor aqueous solubility and dissolution rate to enhance its oral absorption. A central composite design was used to optimise the amount of Poloxamer 188 and D-α-Tocopherol-polyethylene-glycol-succinate (TPGS). The optimised TAC-loaded NLCs contain stearic acid (250 mg), Moringa oleifera (MO) seed oil (50 mg), TAC (Tacrolimus: 10 mg), TPGS (60 mg), and Poloxamer 188 (1% w/v) with a mean diameter of 393.3 ± 29.68 nm, a zeta potential of -18.3 ± 6.19 mV, high entrapment efficiency (92.12 ± 1.14% w/w), and desirability (0.989). TAC-loaded NLCs showed ∼12 times higher drug dissolution efficiency, while in-vitro anti-inflammatory studies showed ∼1.8 times lower IC₅₀ (half-maximal inhibitory concentration) than TAC suspension. The lyophilised TAC-loaded NLCs were found to be stable after 3 months. Thus, the present study concludes the successful encapsulation of TAC in NLCs made of stearic acid and MO seed oil.

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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.