title: Improving oral bioavailability of acyclovir using nanoparticulates of thiolated xyloglucan.
abstract: Acyclovir a BCS class III drug exhibits poor bioavailability due to limited permeability. The intention of this research work was to formulate and characterize thiolated xyloglucan polysaccharide nanoparticles (TH-NPs) of acyclovir with the purpose of increasing its oral bioavailability. Acyclovir-loaded TH-NPs were prepared using a cross-linking agent. Interactions of formulation excipients were reconnoitered using Fourier transform infrared spectroscopy (FT-IR). The formulated nanoparticles were lyophilised by the addition of a cryoprotectant and characterized for its particle size, morphology and stability and optimized using Box Behnken Design.The optimized TH-NP formulation exhibited particle size of 474.4±2.01 and an entrapment efficiency of 81.57%. A marked enhancement in the mucoadhesion was also observed. In-vivo study in a rat model proved that relative bioavailability of acyclovir TH-NPs is ∼2.575 fold greater than that of the marketed acyclovir drug suspension.
authors.affiliation: AISSMS college of Pharmacy, Pune, India. Electronic address: armadgulkar@gmail.com.
authors.forename: Ashwini
authors.initials: A
authors.lastname: Madgulkar
authors.affiliation: AISSMS college of Pharmacy, Pune, India. Electronic address: mrbhalekar@gmail.com.
authors.forename: Mangesh R
authors.initials: MR
authors.lastname: Bhalekar
authors.affiliation: AISSMS college of Pharmacy, Pune, India. Electronic address: amritadikpti@ymail.com.
authors.forename: Amrita A
authors.initials: AA
authors.lastname: Dikpati
mesh_terms: D000212:Acyclovir / Q000737:chemistry* / Q000627:therapeutic use; D000284:Administration, Oral; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000627:therapeutic use; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry / Q000627:therapeutic use; D005936:Glucans / Q000737:chemistry* / Q000627:therapeutic use; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry* / Q000627:therapeutic use; D010316:Particle Size; D051381:Rats; D014990:Xylans / Q000737:chemistry* / Q000627:therapeutic use
chemical_list: D000998:Antiviral Agents; D004337:Drug Carriers; D005936:Glucans; D014990:Xylans; C029353:xyloglucan; D000212:Acyclovir
keywords: Bioavailability; Nanoparticles; Thiolated xyloglucan