冷冻干燥布比卡因脂球:制备、表征和抗微生物特性评估。

IF 2.5 4区 医学 Q3 PHARMACOLOGY & PHARMACY
DARU Journal of Pharmaceutical Sciences Pub Date : 2024-06-01 Epub Date: 2024-02-29 DOI:10.1007/s40199-024-00506-1
Sepehr Labanian, Homa Faghihi, Hamed Montazeri, Aliakbar Jafarian
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引用次数: 0

摘要

目的:制备用于烧伤局部用药的冻干布比卡因脂球。目的是提高其储存稳定性,并开发一种长效释放模式,以解决因频繁使用布比卡因而产生的不良反应:采用热熔分散法制备脂球,以 1.5% 和 3% w/w 的布比卡因为基质,以 6% w/w 的三硬脂苷为核心,以 0.75、1.5 和 3% w/w 的二棕榈酰基磷脂酰胆碱 (DPPC) 和大豆磷脂酰胆碱 (SPC) 为外层。然后对乳液进行冷冻干燥,并用 3% w/w 的蔗糖进行低温保护。通过负载和释放分析、储存研究、颗粒表征(包括形态、ZETA电位和粒度)以及抗微生物评估进行了评估:结果:布比卡因 3% 和 SPC 0.75% 的负载量最高(87.6 ± 0.1%)。在 4 ͦC 下保存 6 个月后,乳液和冻干样品的负载量分别为 17.4 ± 0.2 和 87.2 ± 0.3%。体外溶解试验表明,24 小时后,布比卡因分别从乳液和冻干样品中释放了 94.5% 和 95%。对冻干粉末进行的微观评价显示,其粒径为 35.23 ± 2.02 μm,形态为高度皱缩的不规则状,未发现与药物游离晶体有关的针状结构。该粉末具有快速复溶特性和抗菌活性:冷冻干燥法有望提高布比卡因脂球的贮存稳定性,并能很好地保留释放模式和颗粒特性,以便进一步局部应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Freeze-drying of bupivacaine lipospheres: preparation, characterization, and evaluation of anti-microbial properties.

Purpose: To prepare freeze-dried bupivacaine lipospheres intended for topical application in burn injuries. The aim was improving the storage stability and developing a prolonged release pattern to tackle the adverse reactions resulting from the frequent administration of bupivacaine.

Methods: The lipospheres were prepared by hot-melt dispersion method employing bupivacaine base at 1.5 and 3%w/w, tristearin 6% w/w as the core while dipalmitoyl phosphatidylcholine (DPPC) and soy phosphatidylcholine (SPC) as the coat at 0.75, 1.5 and 3% w/w. The lotion was then freeze-dried and cryoprotected by sucrose 3% w/w. Evaluation was carried out through loading and release analysis, storage study, particle characterization including morphology, zeta potential and particle size as well as anti-microbial assessment.

Results: The highest loading, (87.6 ± 0.1%), was achieved using bupivacaine 3% and SPC 0.75%. After 6 months of storage at 4 ͦC, the loading in the lotion and the freeze-dried samples were 17.4 ± 0.2 and 87.2 ± 0.3%, respectively. In vitro dissolution test demonstrated 94.5% and 95% of bupivacaine release from lotion and freeze-dried samples, after 24 h. The respective zeta potential of -1.30 and 26 mV was recorded for lotion and solid-state bupivacaine. Micromeritic evaluation of freeze-dried powder exhibited particle size of 35.23 ± 2.02 μm and highly-wrinkled-irregular morphology without detectable needle structures related to drug free crystals. The powder had rapid reconstitution property and antibacterial activity.

Conclusion: Freeze- drying holds a promising potential to improve the storage stability of bupivacaine lipospheres with well- preserved release pattern and particle properties for further topical application.

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来源期刊
DARU Journal of Pharmaceutical Sciences
DARU Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-
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期刊介绍: DARU Journal of Pharmaceutical Sciences is a peer-reviewed journal published on behalf of Tehran University of Medical Sciences. The journal encompasses all fields of the pharmaceutical sciences and presents timely research on all areas of drug conception, design, manufacture, classification and assessment. The term DARU is derived from the Persian name meaning drug or medicine. This journal is a unique platform to improve the knowledge of researchers and scientists by publishing novel articles including basic and clinical investigations from members of the global scientific community in the forms of original articles, systematic or narrative reviews, meta-analyses, letters, and short communications.
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