piperidines and carbitol

The solubility values and thermodynamic parameters of a natural phytomedicine/nutrient piperine (PPN) in Transcutol-HP (THP) + water combinations were determined. The mole fraction solubilities (

Topics: Alkaloids; Benzodioxoles; Ethylene Glycols; Piperidines; Polyunsaturated Alkamides; Solubility; Thermodynamics; Water

The objective of present study was to develop and evaluate lipid vesicular transdermal system of iloperidone. Liposomes were prepared successfully using thin film hydration method. With aim of enhancing permeation, cholesterol from liposomes was replaced with transcutol to give PEVs. Liposomes and PEVs were evaluated for particle size, shape, entrapment efficiency, viscosity and release study. The vesicles were incorporated in 0.5% of Carbopol gel and evaluated. Particle size of liposomes and PEVs was found between 200-300 nm and entrapment efficiency was found 80-90%w/w. The transdermal gels were homogeneous, spreadable having acceptable pH and drug content between 90-100%.In ex vivo studies, both liposomes and PEVs showed relatively higher skin deposition and permeation of Iloperidone than the plain drug without vesicles. The in vivo pharmacokinetics studies showed relative bioavailability of the PEV loaded gel as 62% and 166% when compared to the oral drug and gel without vesicles respectively. Pharmacodynamic studies showed FRT and HRT delay responses of the transdermal gel systems were significant[p < 0.05] as compared to control at the end of 24 hs. Thus, it can be concluded that transdermal delivery system can be a promising approach for sustained delivery of Iloperidone.

Topics: Acrylic Resins; Administration, Cutaneous; Animals; Antipsychotic Agents; Biological Availability; Cholesterol; Dermis; Drug Compounding; Ear; Ethylene Glycols; Gels; Isoxazoles; Liposomes; Particle Size; Permeability; Piperidines; Rats; Rats, Wistar; Skin Absorption; Swine

The current studies were undertaken to enhance dissolution and bioavailability/pharmacokinetic profile of a newly approved anticancer drug ibrutinib (IBR) via encapsulation of drug into self-nanoemulsifying drug delivery system (SNEDDS).. Various SNEDDS formulations of IBR were developed by aqueous phase titration method using Capryol-PGMC (oil phase), Tween-20 (surfactant), Carbitol (cosurfactant) and water (aqueous phase). Developed SNEDDS of IBR was evaluated in vitro for various physicochemical properties and drug release profile.. Based on lowest droplet size (28.7 ± 3.2 nm), least polydispersity (0.123), optimal values of zeta potential (-32.8 mV) and refractive index (1.336), highest % transmittance (98.7 ± 0.2%), highest drug release profile via dialysis membrane (98.9 ± 8.2% after 48 h) and the presence of lowest concentration of Capryol-PGMC (12% w/w), SNEDDS I1 was selected for in-vivo pharmacokinetic/bioavailability studies in female Wistar rats. In-vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension. The bioavailability of IBR from optimized SNEDDS I1 was enhanced around 2.64 times in comparison with IBR suspension.. These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy.

Topics: Adenine; Administration, Oral; Animals; Antineoplastic Agents; Biological Availability; Drug Carriers; Drug Compounding; Emulsions; Ethylene Glycols; Female; Nanoparticles; Nanotechnology; Particle Size; Piperidines; Polymers; Polysorbates; Propylene Glycols; Protein Kinase Inhibitors; Pyrazoles; Pyrimidines; Rats, Wistar; Solubility; Surface-Active Agents; Technology, Pharmaceutical; Water