title: Encapsulation and modified-release of thymol from oral microparticles as adjuvant or substitute to current medications.
abstract: The aim of this study was to encapsulate, thymol, in natural polymers in order to obtain (i) taste masking effect and, then, enhancing its palatability and (ii) two formulations for systemic and local delivery of herbal drug as adjuvants or substitutes to current medications to prevent and treat several human and animal diseases. Microspheres based on methylcellulose or hydroxypropyl methylcellulose phthalate (HPMCP) were prepared by spray drying technique. Microparticles were in vitro characterized in terms of yield of production, drug content and encapsulation efficiency, particle size, morphology and drug release. Both formulations were in vivo orally administered and pharmacokinetic analysis was carried 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 remarkably increases compared to the free thymol. In contrast, enteric formulation based on HPMCP shows very limited systemic absorption. These formulations could be proposed as alternative or adjuvants for controlling pathogen infections in human or animal. In particular, methylcellulose microspheres can be used for thymol systemic administration at low doses and HPMCP particles for local treatment of intestinal infections.
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Rassu
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Nieddu
authors.affiliation: Department of Agri-Food Science and Technologies (DISTAL), University of Bologna, 42123 Reggio Emilia, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Bosi
authors.affiliation: Department of Agri-Food Science and Technologies (DISTAL), University of Bologna, 42123 Reggio Emilia, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Trevisi
authors.affiliation: Department of Agri-Food Science and Technologies (DISTAL), University of Bologna, 42123 Reggio Emilia, Italy.
authors.forename: M
authors.initials: M
authors.lastname: Colombo
authors.affiliation: Department of Agri-Food Science and Technologies (DISTAL), University of Bologna, 42123 Reggio Emilia, Italy.
authors.forename: D
authors.initials: D
authors.lastname: Priori
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Manconi
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
authors.forename: P
authors.initials: P
authors.lastname: Giunchedi
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy.
authors.forename: E
authors.initials: E
authors.lastname: Gavini
authors.affiliation: Department of Chemistry and Pharmacy, University of Sassari, 07100 Sassari, Italy. Electronic address: gboatto@uniss.it.
authors.forename: G
authors.initials: G
authors.lastname: Boatto
mesh_terms: D000277:Adjuvants, Pharmaceutic / Q000737:chemistry*; D000818:Animals; D003106:Colon / Q000378:metabolism; D004339:Drug Compounding; D065546:Drug Liberation; D007413:Intestinal Mucosa / Q000378:metabolism; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008863:Microspheres; D010316:Particle Size; D013552:Swine; D013943:Thymol / Q000493:pharmacokinetics*
chemical_list: D000277:Adjuvants, Pharmaceutic; D013943:Thymol; D008747:Methylcellulose; C053309:hydroxypropyl methylcellulose phthalate
keywords: Anti-infective formulations; Herbal drug encapsulation; In vivo studies; Microparticles; Modified-release formulation; Thymol