IMPROVED CHARACTERISTICS OF GLIBENCLAMIDE AS TRANSETHOSOME VESICULAR SYSTEM: PHYSICOCHEMICAL, SOLUBILITY AND IN VITRO PERMEATION STUDY

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI:10.22159/ijap.2024v16i1.49245

Nurul Arfiyanti Yusuf, M. Abdassah, I. Sopyan, R. Mauludin, I. Joni, A. Chaerunisaa

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引用次数: 0

Abstract

Objective: Transethosome as a vesicular system offers high skin permeation; therefore, it is expected to improve the solubility and permeability of the poorly soluble drug glibenclamide. The study aimed to optimize the effect of lipid and surfactant concentration as well as sonication time on the physical characteristics of glibenclamide-loaded transethosomes. Methods: The transethosomes were prepared by solvent evaporation method. An experimental Box-Behnken design optimized the formula by assessing particle size, polydispersity index, zeta potential, and entrapment efficiency as response parameters. Further characterizations were conducted by determining the morphology by TEM, chemical interaction by FTIR, thermal behavior by DSC, as well as solubility improvement by using in vitro drug release and permeation study. Results: The result showed that the optimal formula was that with the lipid composition of 75 mg of soya lecithin, 5 mg of tween 80 as surfactant at a sonication time of 18.79 min. The responses were particle size of 166.8±5.3 nm, polydispersity index of 0.463±0.1, zeta potential of-44.7±2.2 mV, and entrapment efficiency as much as 87.18±3.8%. Glibenclamide-loaded transethosomes exhibited a spherical morphology with no visible aggregation. FTIR study revealed no chemical interactions between Glibenclamide and the excipients. Solubility and in vitro drug release tests showed a significant increase of Glibenclamide from transethosome (p<0.05) compared with that as a bulk powder. Conclusion: Overall, the optimized glibenclamide-loaded transethosomes designed with Box Behnken resulted in improved physicochemical characteristics and increased solubility and drug release compared with that from ethosomes and bulk powder comparison, which will be promising for Glibenclamide to be formulated as transdermal drug delivery.

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改进的格列本脲转乙酰囊泡系统特性：理化、溶解度和体外渗透研究

目的反溶酶体作为一种囊泡系统具有较高的皮肤渗透性，因此有望改善格列本脲这种溶解性较差药物的溶解度和渗透性。本研究旨在优化脂质和表面活性剂浓度以及超声时间对格列本脲转运体物理特性的影响：方法：采用溶剂蒸发法制备反式硫代糖体。方法：采用溶剂蒸发法制备了反式硫体，并通过评估粒度、多分散指数、ZETA电位和夹持效率等响应参数，采用Box-Behnken实验设计优化了配方。进一步的表征包括用 TEM 测定形态、用 FTIR 测定化学作用、用 DSC 测定热行为，以及用体外药物释放和渗透研究来改善溶解度：结果表明，最佳配方是在超声时间为 18.79 分钟时，脂质成分为 75 毫克大豆卵磷脂和 5 毫克吐温 80（表面活性剂）。结果表明，其粒径为 166.8±5.3 nm，多分散指数为 0.463±0.1，zeta 电位为-44.7±2.2 mV，夹带效率高达 87.18±3.8%。装载格列本脲的反式硫体呈球形，无明显聚集。傅立叶变换红外光谱研究表明，格列本脲与辅料之间没有化学作用。溶解度和体外药物释放测试表明，与散装粉末相比，反式硫糖体中的格列本脲含量显著增加（p<0.05）：总之，与乙素体和散装粉末相比，用 Box Behnken 设计的优化的格列本脲负载反式乙素体改善了理化特性，提高了溶解度和药物释放率，这将有望用于格列本脲的透皮给药配方。

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来源期刊

International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

CiteScore

1.40

自引率

0.00%

发文量

219

期刊介绍： International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.