title: In vitro comparative evaluation of monolayered multipolymeric films embedded with didanosine-loaded solid lipid nanoparticles: a potential buccal drug delivery system for ARV therapy.
abstract: Drug delivery via the buccal route has emerged as a promising alternative to oral drug delivery. Didanosine (DDI) undergoes rapid degradation in the gastrointestinal tract, has a short half-life and low oral bioavailability, making DDI a suitable candidate for buccal delivery. Recent developments in buccal drug delivery show an increased interest toward nano-enabled delivery systems. The advantages of buccal drug delivery can be combined with that of nanoparticulate delivery systems to provide a superior delivery system. The aim of this study was to design and evaluate the preparation of novel nano-enabled films for buccal delivery of DDI. Solid lipid nanoparticles (SLNs) were prepared via hot homogenization followed by ultrasonication and were characterized before being incorporated into nano-enabled monolayered multipolymeric films (MMFs). Glyceryl tripalmitate with Poloxamer 188 was identified as most suitable for the preparation of DDI-loaded SLNs. SLNs with desired particle size (PS) (201 nm), polydispersity index (PDI) (0.168) and zeta potential (-18.8 mV) were incorporated into MMFs and characterized. Conventional and nano-enabled MMFs were prepared via solvent casting/evaporation using Eudragit RS100 and hydroxypropyl methylcellulose. Drug release from the nano-enabled films was found to be faster (56% versus 20% in first hour). Conventional MMFs exhibited higher mucoadhesion and mechanical strength than nano-enabled MMFs. SLNs did not adversely affect the steady state flux (71.63 ± 13.54 µg/cm(2) h versus 74.39 ± 15.95 µg/cm(2) h) thereby confirming the potential transbuccal delivery of DDI using nano-enabled MMFs. Nano-enabled buccal films for delivery of DDI can be successfully prepared, and these physico-mechanical studies serve as a platform for future formulation optimization work in this emerging field.
authors.affiliation: Discipline of Pharmaceutical Sciences, School of Health Sciences, University of KwaZulu-Natal , Durban , South Africa.
authors.forename: Elsabé
authors.initials: E
authors.lastname: Jones
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Ojewole
authors.forename: Rahul
authors.initials: R
authors.lastname: Kalhapure
authors.forename: Thirumala
authors.initials: T
authors.lastname: Govender
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D019380:Anti-HIV Agents / Q000008:administration & dosage*; D002626:Chemistry, Pharmaceutical; D016049:Didanosine / Q000008:administration & dosage*; D016503:Drug Delivery Systems; D055119:Elastic Modulus; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000648:ultrastructure; D010316:Particle Size; D010539:Permeability; D020442:Poloxamer / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D013718:Tensile Strength; D014280:Triglycerides / Q000737:chemistry
chemical_list: D019380:Anti-HIV Agents; D008055:Lipids; D011108:Polymers; D014280:Triglycerides; D020442:Poloxamer; C005859:tripalmitin; D016049:Didanosine