title: In vivo evaluation of the vaginal distribution and retention of a multi-particulate pellet formulation.
abstract: Non-disintegrating microcrystalline cellulose pellets (MCC) and disintegrating starch-based pellets were evaluated as new vaginal drug delivery forms and compared with a powder formulation. Pellets and powder were packed in a HPMC or hard gelatine capsule and vaginally administered to five series of five healthy volunteers. Distribution and retention of the multi-particulate formulation was monitored by colposcopy and swabbing. Capsule disintegration in the vagina was slow. MCC pellets clustered around the fornix 3h after administration, and after 24h only a few pellets were detected in the vaginal cavity. In contrast, starch-based pellets already started to disintegrate 6h after administration, resulting in a complete coverage of the vaginal mucosa after 24h in 8 out of 10 volunteers. The powder formulation had a better distribution after 6h, although after 24h almost no powder remained in the vagina. These results were confirmed by swabbing to determine the amount of riboflavin sodium phosphate (used as marker) distributed in the different vaginal regions.
authors.affiliation: Laboratory of Pharmaceutical Technology, Ghent University, Ghent 9000, Belgium.
authors.forename: Nele
authors.initials: N
authors.lastname: Poelvoorde
authors.forename: Hans
authors.initials: H
authors.lastname: Verstraelen
authors.forename: Rita
authors.initials: R
authors.lastname: Verhelst
authors.forename: Bart
authors.initials: B
authors.lastname: Saerens
authors.forename: Ellen
authors.initials: E
authors.lastname: De Backer
authors.forename: Guido Lopes
authors.initials: GL
authors.lastname: dos Santos Santiago
authors.forename: Chris
authors.initials: C
authors.lastname: Vervaet
authors.forename: Mario
authors.initials: M
authors.lastname: Vaneechoutte
authors.forename: Fabienne
authors.initials: F
authors.lastname: De Boeck
authors.forename: Luc
authors.initials: L
authors.lastname: Van Bortel
authors.forename: Marleen
authors.initials: M
authors.lastname: Temmerman
authors.forename: Jean-Paul
authors.initials: JP
authors.lastname: Remon
mesh_terms: D000282:Administration, Intravaginal; D002214:Capsules; D002482:Cellulose / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003127:Colposcopy; D004337:Drug Carriers; D004339:Drug Compounding; D005260:Female; D005486:Flavin Mononucleotide / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D005780:Gelatin / Q000737:chemistry; D006801:Humans; D065347:Hypromellose Derivatives; D007700:Kinetics; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009092:Mucous Membrane / Q000378:metabolism; D017060:Patient Satisfaction; D011208:Powders; D012995:Solubility; D013213:Starch / Q000737:chemistry*; D014621:Vagina / Q000378:metabolism
chemical_list: D002214:Capsules; D004337:Drug Carriers; D011208:Powders; D065347:Hypromellose Derivatives; D005486:Flavin Mononucleotide; D005780:Gelatin; D002482:Cellulose; D008747:Methylcellulose; D013213:Starch; C109691:microcrystalline cellulose