经皮给药阿托伐他汀钙的体贴的开发：体外和体内研究。

IF 3.7 3区医学 Q2 CHEMISTRY, MEDICINAL

Journal of pharmaceutical sciences Pub Date : 2025-02-11 DOI:10.1016/j.xphs.2025.02.001

Pramulani Mulya Lestari , Yahdiana Harahap , Melva Louisa , Silvia Surini

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引用次数: 0

摘要

阿托伐他汀钙是一种生物利用度低的抗高脂血症药物，为了解决这一局限性，研究人员开发了一种利用转运体作为载体的透皮给药系统。本研究旨在提高阿托伐他汀钙的生物利用度，从口服过渡到透皮给药。从粒径、PDI、zeta电位、变形指数和形态等方面观察了六种不同配方的转座体。此外，还观察了该贴片的特性、渗透、药代动力学和刺激性研究。结果表明，阿托伐他汀钙转运体粒径≤130.59 nm， PDI和zeta电位值分别≤0.24和≥-51.87 mV。所制备的囊泡具有球形形态和良好的变形指数。获得的转座体贴片pH值为5.7，粘度值≥8741 m。,分别。经观察，贴载的转座体的粒径≤249.83 nm， zeta电位≥-44.73 mV。通过对阿托伐他汀钙转运体贴剂的渗透研究，发现其具有较高的通量，特别是G6配方，提高了3.67倍的生物利用度，且无刺激性。综上所述，开发经皮给药贴是提高阿托伐他汀钙生物利用度的有效方法。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Development of transethosomes patch for delivery atorvastatin calcium transdermally: In vitro and in vivo studies

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Development of transethosomes patch for delivery atorvastatin calcium transdermally: In vitro and in vivo studies

Atorvastatin calcium is an antihyperlipidemic with low bioavailability, and to address this limitation, a transdermal delivery system utilizing transethosomes as a carrier was developed. This study aimed to enhance the bioavailability of atorvastatin calcium by transitioning from oral to transdermal administration. The six different formulas of transethosomes were observed based on particle size, PDI, zeta potential, deformability index, and morphology. Furthermore, the patch's characteristics, penetration, pharmacokinetic, and irritation studies of transethosomes patch were observed. The results showed that atorvastatin calcium transethosomes had a particle size of ≤ 130.59 nm with PDI and zeta potential values of ≤ 0.24 and ≥ −51.87 mV, respectively. The vesicles featured spherical morphology and an excellent deformability index. The transethosome patches obtained had a pH and viscosity value of 5.7 and ≥ 8741 mPa.s, respectively. The properties of transethosomes loaded in the patch were observed to show a particle size of ≤ 249.83 nm and zeta potential ≥ −44.73 mV. A penetration study of the atorvastatin calcium transethosomes patch reveals high flux, especially the G6 formula, increasing bioavailability by 3.67-fold and not irritating. In conclusion, developing a transethosomes patch for transdermal delivery proved to be an effective method for enhancing the bioavailability of atorvastatin calcium.

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来源期刊

Journal of pharmaceutical sciences 医学-化学综合

CiteScore

7.30

自引率

13.20%

发文量

367

审稿时长

33 days

期刊介绍： The Journal of Pharmaceutical Sciences will publish original research papers, original research notes, invited topical reviews (including Minireviews), and editorial commentary and news. The area of focus shall be concepts in basic pharmaceutical science and such topics as chemical processing of pharmaceuticals, including crystallization, lyophilization, chemical stability of drugs, pharmacokinetics, biopharmaceutics, pharmacodynamics, pro-drug developments, metabolic disposition of bioactive agents, dosage form design, protein-peptide chemistry and biotechnology specifically as these relate to pharmaceutical technology, and targeted drug delivery.