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用作局部给药系统的载盐酸克林霉素去酯化低甲氧基芒果皮果胶膜的制备

Preparation of Clindamycin Hydrochloride Loaded De-Esterified Low-Methoxyl Mango Peel Pectin Film Used as a Topical Drug Delivery System.

作者信息

Chaiwarit Tanpong, Rachtanapun Pornchai, Kantrong Nutthapong, Jantrawut Pensak

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.

Division of Packaging Technology, School of Agro-Industry, Faculty of Agro-Industry, Chiang Mai University, Chiang Mai 50100, Thailand.

出版信息

Polymers (Basel). 2020 Apr 27;12(5):1006. doi: 10.3390/polym12051006.

Abstract

In this study, we aimed to develop a low-mexthoxyl pectin (LMP) from mango peel pectin through a de-esterification method for use as a film forming agent. The prepared de-esterified pectin (DP) was compared to commercial LMP (cLMP) which possessed a 29% degree of esterification (DE). Mango peel pectin was extracted from ripe Nam Dokmai mango peel using the microwave-assisted extraction method. Pectin derived from the mango peel was classified as a high mexthoxyl pectin (79% DE) with 75% of galacturonic acid (GalA) content. A de-esterification experiment was designed by central composite design to plot the surface response curve. Our prepared DP was classified as LMP (DE 29.40%) with 69% GalA. In addition, the Fourier-transform infrared spectrophotometer (FTIR) spectra of the DP were similar to cLMP and the pectin backbone was not changed by the de-esterification process. Strikingly, the cLMP and DP films showed non-significant differences between their physical properties ( > 0.05) with respect to the puncture strength (13.72 N/mm and 11.13 N/mm for the cLMP and DP films, respectively), percent elongation (2.75% and 2.52% for the cLMP and DP films, respectively), and Young's modulus (67.69 N/mm and 61.79 N/mm for the cLMP and DP films, respectively). The de-esterified pectin containing clindamycin HCl (DPC) and low-methoxyl pectin containing clindamycin HCl (cLMPC) films demonstrated 93.47% and 98.79% of drug loading content. The mechanical properties of the cLMPC and DPC films were improved possibly due to their crystal structures and a plasticizing effect of clindamycin HCl loaded into the films. The DPC film exhibited a drug release profile similar to that of the cLMPC film. Our anti-bacterial test of the films found that the cLMPC film showed 41.11 and 76.30 mm inhibitory clear zones against Staphylococcus aureus and Cutibacterium acnes, respectively. The DPC film showed 40.78 and 74.04 mm clear zones against S. aureus and C. acnes, respectively. The antibacterial activities of the cLMPC and DPC films were not significantly different from a commercial clindamycin solution. The results of this study suggest that mango peel pectin can be de-esterified and utilized as an LMP and the de-esterified pectin has the potential for use as a film forming agent, similar to cLMP. In addition, the remarkable use of de-esterified mango peel pectin to prepare films, as shown by our study, holds a great promise as an alternative material for anti-bacterial purposes.

摘要

在本研究中,我们旨在通过脱酯方法从芒果皮果胶中开发一种低甲氧基果胶(LMP),用作成膜剂。将制备的脱酯果胶(DP)与具有29%酯化度(DE)的商业LMP(cLMP)进行比较。采用微波辅助提取法从成熟的南多迈芒果皮中提取芒果皮果胶。从芒果皮中提取的果胶被归类为高甲氧基果胶(DE为79%),半乳糖醛酸(GalA)含量为75%。通过中心复合设计进行脱酯实验以绘制表面响应曲线。我们制备的DP被归类为LMP(DE为29.40%),GalA含量为69%。此外,DP的傅里叶变换红外光谱仪(FTIR)光谱与cLMP相似,并且脱酯过程未改变果胶主链。令人惊讶的是,cLMP和DP薄膜在物理性能方面(>0.05)无显著差异,穿刺强度分别为13.72 N/mm(cLMP薄膜)和11.13 N/mm(DP薄膜),伸长率分别为2.75%(cLMP薄膜)和2.52%(DP薄膜),杨氏模量分别为67.69 N/mm(cLMP薄膜)和61.79 N/mm(DP薄膜)。含盐酸克林霉素的脱酯果胶(DPC)薄膜和含盐酸克林霉素的低甲氧基果胶(cLMPC)薄膜的载药量分别为93.47%和98.79%。cLMPC和DPC薄膜的机械性能可能因其晶体结构以及负载到薄膜中的盐酸克林霉素的增塑作用而得到改善。DPC薄膜表现出与cLMPC薄膜相似的药物释放曲线。我们对薄膜的抗菌测试发现,cLMPC薄膜对金黄色葡萄球菌和痤疮丙酸杆菌的抑菌圈分别为41.11和76.30 mm。DPC薄膜对金黄色葡萄球菌和痤疮丙酸杆菌的抑菌圈分别为40.78和74.04 mm。cLMPC和DPC薄膜的抗菌活性与市售克林霉素溶液无显著差异。本研究结果表明,芒果皮果胶可以脱酯并用作LMP,脱酯果胶有潜力用作成膜剂,与cLMP类似。此外,如我们的研究所表明的,脱酯芒果皮果胶在制备薄膜方面的显著用途有望成为抗菌用途的替代材料。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9597/7284784/2bd9391755db/polymers-12-01006-g001.jpg

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