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聚己内酯/聚（3-羟基丁酸酯-co-3-羟基戊酸酯）微粒作为盐酸马尼地平口服控释的创新载体。

PCL/PHBV microparticles as innovative carriers for oral controlled release of manidipine dihydrochloride.

作者信息

Barboza Fernanda Malaquias, Machado Willian Moreira, Olchanheski Junior Luiz Renato, Padilha de Paula Josiane, Zawadzki Sônia Faria, Fernandes Daniel, Farago Paulo Vitor

机构信息

Laboratory of Pharmaceutical Products, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.

Laboratory of Cardiovascular Pharmacology, Postgraduate Program in Pharmaceutical Science, Department of Pharmaceutical Sciences, State University of Ponta Grossa, 4748 Carlos Cavalcanti Avenue, 84030-900 Ponta Grossa, PR, Brazil.

出版信息

ScientificWorldJournal. 2014 Jan 16;2014:268107. doi: 10.1155/2014/268107. eCollection 2014.

DOI:10.1155/2014/268107
PMID:24550699
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3914481/
Abstract

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization. In vitro dissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulation PCL-M5 was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulation PCL-M5 as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.

摘要

通过简单的乳液/溶剂蒸发法成功制备了含有盐酸马尼地平（MAN）的聚（ε-己内酯）（PCL）和聚（3-羟基丁酸酯-co-3-羟基戊酸酯）（PHBV）微粒。所有制剂的载药效率均大于80%，平均粒径小于8μm。PCL和PHBV制剂分别呈球形，表面光滑且有孔隙。根据傅里叶变换红外光谱，微囊化过程中初始成分未发生化学改性。X射线衍射图谱和差示扫描量热法表明，该过程导致药物非晶化。体外溶出研究表明，所有微粒均延长了MAN的释放，主要是载药量为5%的PCL微粒（PCL-M5）。动物研究表明，制剂PCL-M5在给予去氧肾上腺素后能够使平均动脉压的变化维持长达24小时。这些数据证实了所研究微粒的持续降压作用。结果为将制剂PCL-M5用作口服控释MAN治疗高血压的可行载体提供了实验依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/56a6421fb1ca/TSWJ2014-268107.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/8c6912058bff/TSWJ2014-268107.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/258e01f471a0/TSWJ2014-268107.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/343c37f67ac4/TSWJ2014-268107.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/62c9dde7b050/TSWJ2014-268107.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/8c8343dd145e/TSWJ2014-268107.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/79e019183daf/TSWJ2014-268107.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/81c6c688a7d2/TSWJ2014-268107.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/56a6421fb1ca/TSWJ2014-268107.008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/8c6912058bff/TSWJ2014-268107.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/258e01f471a0/TSWJ2014-268107.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/343c37f67ac4/TSWJ2014-268107.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/62c9dde7b050/TSWJ2014-268107.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/8c8343dd145e/TSWJ2014-268107.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/79e019183daf/TSWJ2014-268107.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/81c6c688a7d2/TSWJ2014-268107.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0dfb/3914481/56a6421fb1ca/TSWJ2014-268107.008.jpg

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