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Encapsulation and modified-release of thymol from oral microparticles as adjuvant or substitute to current medications

Rassu, Giovanna and Nieddu, Maria and Bosi, Paolo and Trevisi, Paolo and Colombo, M.M. and Priori, D. and Manconi, Paola Maria and Giunchedi, Paolo and Gavini, Elisabetta and Boatto, Gianpiero (2014) Encapsulation and modified-release of thymol from oral microparticles as adjuvant or substitute to current medications. Phytomedicine, Vol. 21 (12), p. 1627-1632. ISSN 0944-7113. eISSN 1618-095X. Article.

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DOI: 10.1016/j.phymed.2014.07.017

Abstract

The aim of this study was to encapsulate, thymol, in natural polymers in order to obtain (i) taste mask-ing effect and, then, enhancing its palatability and (ii) two formulations for systemic and local deliveryof herbal drug as adjuvants or substitutes to current medications to prevent and treat several humanand animal diseases. Microspheres based on methylcellulose or hydroxypropyl methylcellulose phtha-late (HPMCP) were prepared by spray drying technique. Microparticles were in vitro characterized interms of yield of production, drug content and encapsulation efficiency, particle size, morphology anddrug release. Both formulations were in vivo orally administered and pharmacokinetic analysis wascarried out. The polymers used affect the release and, then, the pharmacokinetic profile of thymol. Encapsulation into methylcellulose microspheres leads to short half/life but bioavailability remarkablyincreases compared to the free thymol. In contrast, enteric formulation based on HPMCP shows verylimited systemic absorption. These formulations could be proposed as alternative or adjuvants for con-trolling pathogen infections in human or animal. In particular, methylcellulose microspheres can be usedfor thymol systemic administration at low doses and HPMCP particles for local treatment of intestinalinfections.

Item Type:Article
ID Code:10636
Status:Published
Refereed:Yes
Uncontrolled Keywords:Thymol, herbal drug encapsulation, anti-infective formulations, microparticles, modified-release formulation, in vivo studies
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Urban & Fischer / Elsevier
ISSN:0944-7113
eISSN:1618-095X
Deposited On:16 Jan 2015 13:06

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