Effects of counteranion of TRH and loading amount on control of TRH release from copoly(dl-lactic/glycolic acid) microspheres prepared by an in-water drying method

Heya Toshiro, Okada Hiroaki, Tanigawara Yusuke, Ogawa Yasuaki, Toguchi Hajime

研究成果: Article査読

66 被引用数 (Scopus)

抄録

The preparation of injectable sustained release microspheres of TRH was investigated. The drug was encapsulated in copoly(dl-lactic/glycolic acid) (PLGA) using an in-water drying method through a w/o/w emulsion. The predominant factors influencing the entrapment ratio of TRH in the microspheres and the release rate of TRH from the microspheres were the loading amount and the dissociation state of the drug. Microspheres of TRH encapsulated as a free base at an adequate concentration provided a small initial burst followed by a zero-order prolonged release regardless of the high water solubility of the drug. The addition of strong acids to the inner aqueous phase interfered with the encapsulation efficacy and caused a large initial burst. The ionic interaction between the basic functional group of TRH and the carboxylic acid end group of PLGA during the preparation is necessary to produce a rigid matrix of the microspheres. This method is applicable to the microencapsulation of other water-soluble basic peptides in PLGA.

本文言語English
ページ(範囲)69-75
ページ数7
ジャーナルInternational Journal of Pharmaceutics
69
1
DOI
出版ステータスPublished - 1991 2月 15
外部発表はい

ASJC Scopus subject areas

  • 薬科学

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