title: Enhanced gastric tolerability and improved anti-obesity effect of capsaicinoids-loaded PCL microparticles.
abstract: Capsaicinoids show several pharmacological effects including weight loss. However, their pungency limits the long-term use through the gastrointestinal tract. In that sense, the goal of this study was to prepare capsaicinoids-loaded poly(ε-caprolactone) microparticles as an oral carrier in order to improve their gastric tolerability and to make feasible the long-term treatment of obesity. Formulations containing 3, 5 and 10% capsaicinoids were successfully obtained by simple emulsion/solvent evaporation method. Values of encapsulation efficiency above 90% were achieved. Microparticles showed spherical shape and smooth surface. The particle size was suitable for oral use in order to provide an extended release through the gastrointestinal tract. No chemical bond was observed between drug and polymer. Microencapsulation led to drug amorphization. Formulations prolonged the release of capsaicinoids without changing the release kinetic (biexponential model). Microencapsulation increased the gastric tolerability of capsaicinoids because it prevented inflammatory processes in the stomach of rats. Microparticles containing 5% capsaicinoids demonstrated a statistically significant reduction of Lee index, mesenteric and retroperitoneal fat pads of rats with obesity induced by hypothalamic lesion using monosodium l-glutamate. In summary, capsaicinoids-loaded poly(ε-caprolactone) microparticles are low-irritative oral controlled-release carriers for a long-term use in obesity.
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Martinha A
authors.initials: MA
authors.lastname: Almeida
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Jessica M
authors.initials: JM
authors.lastname: Nadal
authors.affiliation: Department of General Biology, State University of Ponta Grossa, Brazil.
authors.forename: Sabrina
authors.initials: S
authors.lastname: Grassiolli
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Katia S
authors.initials: KS
authors.lastname: Paludo
authors.affiliation: Department of Chemistry, Federal University of Paraná, Brazil.
authors.forename: Sônia F
authors.initials: SF
authors.lastname: Zawadzki
authors.affiliation: Department of Industrial Pharmacy, Federal University of Santa Maria, Brazil.
authors.forename: Letícia
authors.initials: L
authors.lastname: Cruz
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Josiane P
authors.initials: JP
authors.lastname: Paula
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, State University of Ponta Grossa, Brazil. Electronic address: pvfarago@gmail.com.
authors.forename: Paulo V
authors.initials: PV
authors.lastname: Farago
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002211:Capsaicin / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004337:Drug Carriers / Q000737:chemistry*; D008863:Microspheres; D009765:Obesity / Q000188:drug therapy; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013270:Stomach / Q000187:drug effects* / Q000473:pathology; D013696:Temperature
chemical_list: D004337:Drug Carriers; D011091:Polyesters; C016240:polycaprolactone; D002211:Capsaicin
keywords: Capsaicin; Controlled-release carriers; Dihydrocapsaicin; Low-irritative oral preparation; Poly(ε-caprolactone); Weight-loss strategy