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Local sustained delivery of bupivacaine HCl from a new castor oil-based nanoemulsion system.
Rachmawati, Heni; Arvin, Yang Aryani; Asyarie, Sukmadjaja; Anggadiredja, Kusnandar; Tjandrawinata, Raymond Rubianto; Storm, Gert.
Afiliación
  • Rachmawati H; School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia. h_rachmawati@fa.itb.ac.id.
  • Arvin YA; Research Center for Nanosciences and Nanotechnology, Ganesha 10, Bandung, 40132, Indonesia. h_rachmawati@fa.itb.ac.id.
  • Asyarie S; School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia.
  • Anggadiredja K; School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia.
  • Tjandrawinata RR; School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia.
  • Storm G; Dexa Laboratories of Biomolecular Sciences, Jababeka, Cikarang, 17530, Indonesia.
Drug Deliv Transl Res ; 8(3): 515-524, 2018 06.
Article en En | MEDLINE | ID: mdl-29516407
ABSTRACT
Bupivacaine HCl (1-butyl-2',6'-pipecoloxylidide hydrochloride), an amide local anesthetic compound, is a local anesthetic drug utilized for intraoperative local anesthesia, post-operative analgesia and in the treatment of chronic pain. However, its utility is limited by the relative short duration of analgesia after local administration (approximately 9 h after direct injection) and risk for side effects. This work is aimed to develop a nanoemulsion of bupivacaine HCl with sustained local anesthetics release kinetics for improved pain management, by exhibiting extended analgesic action and providing reduced peak levels in the circulation to minimize side effects. Herein, biodegradable oils were evaluated for use in nanoemulsions to enable sustained release kinetics of bupivacaine HCl. Only with castor oil, a clear and stable nanoemulsion was obtained without the occurrence of phase separation over a period of 3 months. High loading of bupivacaine HCl into the castor oil-based nanoemulsion system was achieved with about 98% entrapment efficiency and the resulting formulation showed high stability under stress conditions (accelerated stability test) regarding changes in visual appearance, drug content, and droplet size. We show herein that the in vitro release and in vivo pharmacokinetic profiles as well as pharmacodynamic outcome (pain relief test) after subcutaneous administration in rats correlate well and clearly demonstrate the prolonged release and extended duration of activity of our novel nanoformulation. In addition, the lower Cmax value achieved in the blood compartment suggests the possibility that the risk for systemic side effects is reduced. We conclude that castor oil-based nanomulsion represents an attractive pain treatment possibility to achieve prolonged local action of bupivacaine HCl.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Bupivacaína / Aceite de Ricino / Nanoestructuras / Anestésicos Locales Idioma: En Revista: Drug Deliv Transl Res Año: 2018 Tipo del documento: Article País de afiliación: Indonesia

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Bupivacaína / Aceite de Ricino / Nanoestructuras / Anestésicos Locales Idioma: En Revista: Drug Deliv Transl Res Año: 2018 Tipo del documento: Article País de afiliación: Indonesia