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聚焦光束反射测量法在单相乳液体系溶剂蒸发法中制备基于聚乳酸-乙醇酸共聚物的微球中对聚合物类型的影响。

Polymer type effect on PLGA-based microparticles preparation by solvent evaporation method with single emulsion system using focussed beam reflectance measurement.

机构信息

Faculty of Pharmacy, Universitas Padjadjaran, Jatinangor, Indonesia.

College of Pharmacy, Freie Universität Berlin, Berlin, Germany.

出版信息

J Microencapsul. 2022 Sep;39(6):512-521. doi: 10.1080/02652048.2022.2116120. Epub 2022 Sep 10.

DOI:10.1080/02652048.2022.2116120
PMID:36089916
Abstract

AIM

This study aimed to investigate the effect of polymer type on solidification rate of PLGA polymeric microparticles and particle size/distribution of the emulsion droplets/hardened PLGA polymeric microparticles during solvent evaporation process using FBRM (Focussed Beam Reflectance Measurement).

METHODS

PLGA polymeric microparticles were prepared by an O/W solvent evaporation method using various PLGA polymers, including PLGA Resomer® RG503H, RG502H and RG752H. The particle size mean, chord length distribution (CLD), and chord count of the emulsion droplets/hardened microparticles were monitored by FBRM. The morphology of polymeric microparticles were characterised by optical microscopy and scanning electron microscopy (SEM).

RESULTS

The transformation of the emulsion droplets into solid microparticles occurred within the first 30 (± 1.04), 34 (± 1.15) and 37 (± 0.82) min and square weighted mean chord lengths are 64.08 (± 3.18), 52.36 (± 5.27) and 42.18 (± 4.61) µm when PLGA Resomer® RG503H, RG502H and RG752H were used respectively. Larger square weighted mean chord length of PLGA polymeric microparticles gave lower chord counts. PLGA RG752H microparticles gave smallest square weighted mean chord length and the chord counts was the highest. The CLDs measured by FBRM showed that a larger particle size mean gave longer CLD and a lower peak of particle number. SEM data revealed that the morphology of microparticles was influenced by type and physical properties of polymer.

CONCLUSIONS

FBRM can be employed for online monitoring of the shift in the microparticle CLD and detect transformation of the emulsion droplets into solid microparticles during the solvent evaporation process. The microparticle CLD and transformation process were strongly influenced by polymer type.

摘要

目的

本研究旨在使用 FBRM(聚焦光束反射测量)研究聚合物类型对 PLGA 聚合物微球的固化速率和乳液液滴/固化 PLGA 聚合物微球的粒径/分布的影响。

方法

使用各种 PLGA 聚合物(包括 PLGA Resomer® RG503H、RG502H 和 RG752H)通过 O/W 溶剂蒸发法制备 PLGA 聚合物微球。通过 FBRM 监测乳液液滴/固化微球的粒径平均值、弦长分布(CLD)和弦数。使用光学显微镜和扫描电子显微镜(SEM)对聚合物微球的形态进行了表征。

结果

乳液液滴转化为固体微球发生在最初的 30(±1.04)、34(±1.15)和 37(±0.82)分钟内,当使用 PLGA Resomer® RG503H、RG502H 和 RG752H 时,正方形加权平均弦长分别为 64.08(±3.18)、52.36(±5.27)和 42.18(±4.61)μm。PLGA 聚合物微球的较大正方形加权平均弦长导致较低的弦数。PLGA RG752H 微球给出最小的正方形加权平均弦长,并且弦数最高。FBRM 测量的 CLD 表明,较大的粒径平均值给出较长的 CLD 和较低的颗粒数峰值。SEM 数据表明,微球的形态受聚合物类型和物理性质的影响。

结论

FBRM 可用于在线监测微球 CLD 的变化,并在溶剂蒸发过程中检测乳液液滴向固体微球的转化。微球的 CLD 和转化过程受聚合物类型的强烈影响。

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