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通过包裹在粘膜粘附纳米颗粒中进行乙酰唑胺的局部给药。

Topical delivery of acetazolamide by encapsulating in mucoadhesive nanoparticles.

作者信息

Manchanda Satish, Sahoo Pravat Kumar

机构信息

Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), Pushp Vihar Sector III, MB Road, New Delhi 110017, India.

出版信息

Asian J Pharm Sci. 2017 Nov;12(6):550-557. doi: 10.1016/j.ajps.2017.04.005. Epub 2017 May 16.

DOI:10.1016/j.ajps.2017.04.005
PMID:32104368
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7032124/
Abstract

The intent of this study was to provide topical delivery of acetazolamide by preparing chitosan-STPP (sodium tripolyphosphate) nanoparticles of acetazolamide and evaluate the particle size, zeta potential, drug entrapment, particle morphology; drug release and efficacy. The particles showed sustained drug release which followed the Higuchi kinetic model. The results indicate that the nanoparticles released the drug by a combination of dissolution and diffusion. The optimised formulation was having particle size 188.46 ± 8.53 nm and zeta potential + 36.86 ± 0.70 mV. The particles were spherical with a polydispersity index of 0.22 ± 0.00. Powder X-ray diffraction and differential scanning calorimetry indicated diminished crystallinity of drug in the nanoparticle formulation. In the permeation study, the nanoparticle formulation showed elevated permeation as compared to that of drug solution with negative signs of corneal damage. mucoadhesion studies showed 90.34 ± 1.12% mucoadhesion. The studies involving ocular hypotensive activity in rabbits revealed significantly higher hypotensive activity (P < 0.05) as compared with plain drug solution with no signs of ocular irritation. The stability studies revealed that formulation was quite stable.

摘要

本研究的目的是通过制备乙酰唑胺的壳聚糖-三聚磷酸钠（STPP）纳米颗粒来实现乙酰唑胺的局部给药，并评估其粒径、zeta电位、药物包封率、颗粒形态、药物释放和疗效。这些颗粒呈现出符合Higuchi动力学模型的持续药物释放。结果表明，纳米颗粒通过溶解和扩散相结合的方式释放药物。优化后的制剂粒径为188.46±8.53nm，zeta电位为+36.86±0.70mV。颗粒呈球形，多分散指数为0.22±0.00。粉末X射线衍射和差示扫描量热法表明，纳米颗粒制剂中药物的结晶度降低。在渗透研究中，纳米颗粒制剂与药物溶液相比表现出更高的渗透率，且角膜损伤迹象为阴性。粘膜粘附研究显示粘膜粘附率为90.34±1.12%。涉及兔眼降压活性的研究表明，与普通药物溶液相比，降压活性显著更高（P<0.05），且无眼刺激迹象。稳定性研究表明该制剂相当稳定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/095e94e8cd79/ajps438-fig-0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/24850a436dc3/ajps438-ga-5001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/1ca6b807db2f/ajps438-fig-0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/4f9f8ab9799b/ajps438-fig-0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/4057785c6b23/ajps438-fig-0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/558207f9534d/ajps438-fig-0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/6a6873af233a/ajps438-fig-0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/8edc9a335614/ajps438-fig-0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/0b67f5150c1f/ajps438-fig-0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/095e94e8cd79/ajps438-fig-0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/24850a436dc3/ajps438-ga-5001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/1ca6b807db2f/ajps438-fig-0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/4f9f8ab9799b/ajps438-fig-0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/4057785c6b23/ajps438-fig-0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/558207f9534d/ajps438-fig-0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/6a6873af233a/ajps438-fig-0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/8edc9a335614/ajps438-fig-0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/0b67f5150c1f/ajps438-fig-0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6459/7032124/095e94e8cd79/ajps438-fig-0008.jpg

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