Alginate-pectin-poly-L-lysine particulate as a potential controlled release formulation.
Drug delivery particulates were prepared using alginate, polylysine and pectin. Theophylline, chlorothiazide and indomethacin were used as the model drugs for in-vitro assessments, and mannitol was the model for assessing paracellular drug absorption across Caco-2 cell monolayers. Alginate and pectin served as the core polymers and polylysine helped to strengthen the particulates. Use of pectin specially helped in forming a more robust particulate that was more resistant in acidic pH and modulated the release profiles of the encapsulated model drugs in the alkaline pH. Alginate and pectin were also found to enhance the paracellular absorption of mannitol across Caco-2 cell monolayers by about three times. The release rate could be described as a first-order or square-root time process depending on the drug load. Use of alginate-polylysine-pectin particulates is expected to combine the advantages of bioadhesion, absorption enhancement, and sustained release. This particulate system may have potential use as a carrier for drugs that are poorly absorbed after oral administration.
Liu
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P
School of Pharmacy, Memorial University of Newfoundland, St John's, Canada.
Krishnan
T R
TR
D000268:Adhesiveness; D000464:Alginates / Q000008:administration & dosage / Q000648:ultrastructure; D000818:Animals; D018938:Caco-2 Cells; D002214:Capsules; D002740:Chlorothiazide / Q000378:metabolism / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000008:administration & dosage*; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems; D005780:Gelatin; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007213:Indomethacin / Q000378:metabolism / Q000493:pharmacokinetics; D008297:Male; D017348:Microscopy, Electron, Scanning Transmission; D010316:Particle Size; D010368:Pectins / Q000008:administration & dosage / Q000648:ultrastructure; D011107:Polylysine / Q000008:administration & dosage; D051381:Rats; D017208:Rats, Wistar; D013806:Theophylline / Q000378:metabolism / Q000493:pharmacokinetics; D013997:Time Factors
D000464:Alginates; D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D011107:Polylysine; D002740:Chlorothiazide; D010368:Pectins; D020723:Glucuronic Acid; D005780:Gelatin; D013806:Theophylline; D007213:Indomethacin