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Development of poly(lactic-co-glycolic acid) microparticles with pH-sensitive drug release behaviors

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Abstract

We developed a novel pH-sensitive microparticle using poly(lactide-co-glycolide) (PLGA) and 3-diethylaminopropylated poly(l-lysine) [poly(Lys-DEAP)] (pKb of DEAP ~6.5). Here, the design of the microparticle takes advantage of the unique pH-sensitive feature of poly(Lys-DEAP) as either a non-ionic characteristic of DEAP moieties at pH 7.4 or an ionic characteristic of DEAP moieties at acidic pH. In particular, the ionized DEAP in PLGA microparticles modulated acidic pH-activated microparticle-destruction and allowed accelerated release of the encapsulated drug content when the pH of the solution was decreased to from 7.4 to 6.8 or 6.0. We believe that this microparticle system is expected to improve the treatment efficacy for lung diseases with chronic respiratory acidosis.

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Acknowledgments

This article does not contain any studies with human and animal subjects performed by any of the authors. All authors (J.O. Lee, Y.S. Youn, D.K. Lee, K.H. Cha, E.S. Lee) declare that they have no conflict of interest. This work was financially supported by the GRRC program of Gyeonggi-do province [GRRC 2014-B01, Development of industrial nano-/micro-sized biomaterials for high performance drug release control].

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Authors and Affiliations

  1. Department of Biotechnology, The Catholic University of Korea, 43-1 Yeokgok 2-dong, Wonmi-gu, Bucheon, Gyeonggi-do, 420-743, Republic of Korea

    Jung Ok Lee & Eun Seong Lee

  2. College of Pharmacy, SungKyunKwan University, 300 Chonchon-dong, Jangan-ku, Suwon, Gyeonggi-do, 440-746, Republic of Korea

    Yu Seok Youn

  3. Gyeonggi Bio-Center, Dongkook Pharm. Co, Iui-dong, Yeongtong-gu, Suwon, 443-270, Republic of Korea

    Deok-Keun Lee & Kyung-Hoi Cha

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  1. Jung Ok Lee
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  2. Yu Seok Youn
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  3. Deok-Keun Lee
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  4. Kyung-Hoi Cha
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  5. Eun Seong Lee
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Correspondence to Eun Seong Lee.

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Lee, J.O., Youn, Y.S., Lee, DK. et al. Development of poly(lactic-co-glycolic acid) microparticles with pH-sensitive drug release behaviors. Journal of Pharmaceutical Investigation 45, 151–156 (2015). https://doi.org/10.1007/s40005-014-0157-9

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  • DOI: https://doi.org/10.1007/s40005-014-0157-9

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