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Open AccessArticle

Elaboration of Charged Poly(Lactic-co-Glycolic Acid) Microparticles for Effective Release of Tranexamic Acid

1
National Institute of Infectious Diseases and Vaccinology, National Health Research Institutes, Miaoli 35053, Taiwan
2
Department of Chemical Engineering, National United University, Miaoli 36063, Taiwan
3
Ph.D. Program in Materials and Chemical Engineering, National United University, Miaoli 36063, Taiwan
*
Author to whom correspondence should be addressed.
Polymers 2020, 12(4), 808; https://doi.org/10.3390/polym12040808
Received: 16 March 2020 / Revised: 29 March 2020 / Accepted: 30 March 2020 / Published: 4 April 2020
(This article belongs to the Special Issue Polymers and Drug Delivery Systems)
In this study, tranexamic acid (TA) was used as a model compound to study the charge effect on the physicochemical properties of poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs). Charged PLGA MPs were elaborated by the incorporation of a quaternary ammonium, cetyltrimethylammonium bromide (CTAB), during the double emulsion solvent evaporation process. Three TA-CTAB-carrying modes of PLGA MPs were designed in the CTAB-free (TA-MP), adsorption (TA-CTABAD), or encapsulation (TA-CTABEN) form. The obtained MPs were characterized by morphology and TA-MP affinity. The experiment revealed that the three prepared MPs were spherical and smooth, with pores on their surfaces. TA-CTABAD had a relatively narrow size distribution, compared with that of TA-MP and TA-CTABEN. The particle sizes of TA-MP, TA-CTABEN, TA-CTABAD were measured as 59 ± 17, 54 ± 20, and 19 ± 8 μm, respectively. The zeta potential of the three MPs was found to be in the order: TA-CTABAD > TA-CTABEN > TA-MP. Differential scanning calorimetry (DSC) indicated that the manufacturing process had no influence on the glass transition temperature of the MPs, which was close to 48 °C. Thermogravimetric analysis illustrated that the presence of CTAB slightly changed the thermal stability of PLGA MPs. In vitro release showed that TA-CTABAD exhibited faster TA release than TA-MP and TA-CTABEN in a basic environment (pH of 13), probably because of electrostatic attraction. At pH = 1, the release of TA from TA-CTABEN was faster than those from TA-MP and TA-CTABAD, probably because of electrostatic repulsion. However, the effect of electrostatic interaction was not significant at pH = 7.4. View Full-Text
Keywords: poly(lactic-co-glycolic acid); cetyltrimethylammonium bromide; tranexamic acid; controlled release; charge effect poly(lactic-co-glycolic acid); cetyltrimethylammonium bromide; tranexamic acid; controlled release; charge effect
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Huang, M.-H.; Huang, S.-Y.; Chen, Y.-X.; Chen, C.-Y.; Lin, Y.-S. Elaboration of Charged Poly(Lactic-co-Glycolic Acid) Microparticles for Effective Release of Tranexamic Acid. Polymers 2020, 12, 808.

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