Microprocessor in controlled transdermal drug delivery of anti-cancer drugs.
Microprocessor controlled transdermal delivery of anticancer drugs 5-Fluorouracil (5-FU) and 6-Mercaptopurine (6-MP) was developed and in vitro evaluation was done. Drugs were loaded based on the pharmacokinetics parameters. In vitro diffusion studies were carried at different current density (0.0, 0.1, 0.22, 0.50 mA/cm2). The patches were evaluated for the drug content, thickness, weight, folding endurance, flatness, thumb tack test and adhesive properties all were well with in the specification of transdermal patches with elegant and transparent in appearance. In vitro permeation studies through human cadaver skin showed, passive delivery (0.0 mA/cm2) of 6-MP was low. As the current density was progressively increased, the flux also increased. the flux also increased with 0.1 mA/cm2 for 15-20 min, but it was less than desired flux, 0.2 mA/cm2 for 30 min showed better flux than 0.1 mA/cm2 current, but lag time was more than 4 h, 0.5 mA/cm2 current for more than 1 h, flux was >159 microg/cm2 h which was desired flux for 6-MP. 5-FU flux reached the minimum effective concentration (MEC) of 54 microg/cm2 h with 0.5 mA/cm2 current for 30-45 min, drug concentration were within the therapeutic window in post-current phase. We concluded from Ohm's Law that as the resistance decreases, current increases. Skin resistance decrease with increase in time and current, increase in the drug permeation. Interestingly, for all investigated current densities, as soon as the current was switched off, 5-FU and 6-MP flux decreased fairly, but the controlled drug delivery can be achieved by switching the current for required period of time.
Chandrashekar
N S
NS
Department of Pharmaceutics, Al-Ameen College of Pharmacy, Near Lalbagh Main Gate, Hosur Road, Bangalore 560 027, Karnataka, India. nschandrashekar@gmail.com
Shobha Rani
R H
RH
D000279:Administration, Cutaneous; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002102:Cadaver; D003692:Delayed-Action Preparations / Q000008:administration & dosage*; D004058:Diffusion; D016503:Drug Delivery Systems / Q000295:instrumentation* / Q000379:methods; D017097:Electric Impedance; D005472:Fluorouracil / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D015122:Mercaptopurine / Q000008:administration & dosage / Q000493:pharmacokinetics; D008838:Microcomputers; D012867:Skin / Q000378:metabolism / Q000473:pathology; D012869:Skin Absorption / Q000502:physiology
D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D015122:Mercaptopurine; D005472:Fluorouracil