Mucoadhesive Properties of Thiolated Pectin-Based Pellets Prepared by Extrusion-Spheronization Technique.
The aim of this study was to develop mucoadhesive pellets on a thiolated pectin base using the extrusion-spheronization technique. Thiolation of pectin was performed by esterification with thioglycolic acid. The molecular weight and thiol group content of the pectins were determined. Pellets containing pectin, microcrystalline cellulose, and ketoprofen were prepared and their mucoadhesive properties were evaluated through a wash-off test using porcine intestinal mucosa. The in vitro ketoprofen release was also evaluated. Thiolated pectin presented a thiol group content of 0.69 mmol/g. Thiolation caused a 13% increase in polymer molecular weight. Pellets containing thiolated pectin were still adhering to the intestinal mucosa after 480 min and showed a more gradual release of ketoprofen. Conversely, pellets prepared with nonthiolated pectin showed rapid disintegration and detached after only 15 min. It can be concluded that thiolated pectin-based pellets can be considered a potential platform for the development of mucoadhesive drug delivery systems for the oral route.
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
André Luiz Lopes
AL
Martins
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Aline Carlos
AC
de Oliveira
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Carolina Machado Ozório Lopes
CM
do Nascimento
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Luís Antônio Dantas
LA
Silva
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Marilisa Pedroso Nogueira
MP
Gaeti
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Eliana Martins
EM
Lima
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil.
Stephânia Fleury
SF
Taveira
Laboratory of Polymer Chemistry, Department of Biochemistry and Molecular Biology, Institute of Biological Sciences - ICB II, Federal University of Goiás, Goiânia, Brazil.
Kátia Flávia
KF
Fernandes
School of Pharmacy, Federal University of Goiás, Goiânia, Brazil. Electronic address: ricardomarreto@ufg.br.
Ricardo Neves
RN
Marreto
D000269:Adhesives / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004343:Drug Implants / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D007413:Intestinal Mucosa / Q000187:drug effects / Q000378:metabolism; D010368:Pectins; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013552:Swine
D000269:Adhesives; D004343:Drug Implants; D013438:Sulfhydryl Compounds; D010368:Pectins
extrusion; mucoadhesive; oral drug delivery; polymer synthesis; polymeric biomaterials; solid dosage form; spheronization