title: Evaluation of tadalafil nanosuspensions and their PEG solid dispersion matrices for enhancing its dissolution properties.
abstract: The aim of this work was to prepare and evaluate Tadalafil nanosuspensions and their PEG 4000 solid dispersion matrices to enhance its dissolution rate. Nanosuspensions were prepared by precipitation/ultrasonication technique at 5°C where different stabilizers were screened for stabilization. Nanosuspensions were characterized in terms of particle size and charge. Screening process limited suitable stabilizers into structurally related surfactants composed of a mixture of Tween80 and Span80 at 1:1 ratio (in percent, weight/volume) in adjusted alkaline pH (named TDTSp-OH). The surfactant mixture aided the production of nanosuspensions with an average particle size of 193 ± 8 nm and with short-term stability sufficient for further processing. Solid dispersion matrices made of dried Tadalafil nanosuspensions or dried Tadalafil raw powder suspensions and PEG 4000 as a carrier were prepared by direct compression. Drying was performed via dry heat or via freeze dry. Drug release studies showed that, in general, tablet formulations made of freeze-dried product exhibited faster initial release rates than the corresponding tablets made of oven-dried products which could be attributed to possible larger crystal growth and larger crushing strengths of oven-dried formulations. At best, 60% of drug was released from solid dispersion matrices, while more than 90% of drug was released from TDTSp-OH nanosuspension within the first 5 min. In conclusion, Tadalafil nanosuspensions obtained using a mixed surfactant system provided rapid dissolution rates of Tadalafil that can theoretically enhance its bioavailability.
authors.affiliation: Department of Pharmaceutical Technology, Jordan University of Science and Technology, Irbid, 22110, P.O. Box 3030, Jordan, wasfy72@yahoo.com.
authors.forename: Wasfy M
authors.initials: WM
authors.lastname: Obeidat
authors.forename: Al-Sayed A
authors.initials: AS
authors.lastname: Sallam
mesh_terms: D002243:Carbolines / Q000737:chemistry / Q000493:pharmacokinetics*; D004353:Drug Evaluation, Preclinical; D036103:Nanotechnology; D010316:Particle Size; D058986:Phosphodiesterase 5 Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols / Q000737:chemistry*; D012995:Solubility; D000068581:Tadalafil
chemical_list: D002243:Carbolines; D058986:Phosphodiesterase 5 Inhibitors; D011092:Polyethylene Glycols; D000068581:Tadalafil