Acrylate-based transdermal therapeutic system of nitrendipine.
The objective of the present research investigation was to fabricate an acrylate-based transdermal therapeutic system (TTS) of nitrendipine, which could deliver drug at maximum input rate so as to deliver drug in minimum patch size. Transdermal patches were fabricated using synthesized acrylate pressure-sensitive adhesives (PSAs): PSA1, PSA2, and commercially available PSA3 and PSA4 using d-limonene as permeation enhancer. Effect of concentration of d-limonene on permeation kinetics of nitrendipine in PSAs was studied. Fabricated TTS in mentioned PSAs were evaluated for in-vitro release and permeation kinetics through guinea-pig skin. Cumulative release of drug in PSA1, PSA2, PSA3, and PSA4 was observed to be 45%, 40%, 25%, and 25%, respectively, upto 24 hr. Flux of drug through guinea-pig skin calculated at 48 hr in PSA1, PSA2, PSA3, and PSA4, with and without d-limonene, was observed to be 0.346+/-0.10, 0.435+/-0.17, 0.410+/-0.17, and 0.162+/-0.06, and 0.625+/-0.19, 1.161+/-0.46, 0.506+/-0.17, and 0.520+/-0.18 (microg/cm2/hr), respectively. The TTS in PSA2 showed comparatively high flux and could deliver drug at high input rate through transdermal route. PSA2 was found to have good rate-controlling property and could be successfully employed in transdermal delivery of nitrendipine.
Tipre
Dnyanesh N
DN
University Department of Chemical Technology, Pharmaceutical Division, University of Mumbai, Matunga, Mumbai, India.
Vavia
Pradeep R
PR
D000179:Acrylates / Q000737:chemistry*; D000269:Adhesives; D000277:Adjuvants, Pharmaceutic; D000279:Administration, Cutaneous; D000818:Animals; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics; D053138:Cyclohexenes; D003692:Delayed-Action Preparations; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D000077222:Limonene; D008297:Male; D009568:Nitrendipine / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D010539:Permeability; D011108:Polymers; D011312:Pressure; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012997:Solvents; D013729:Terpenes; D013997:Time Factors
D000179:Acrylates; D000269:Adhesives; D000277:Adjuvants, Pharmaceutic; D002121:Calcium Channel Blockers; D053138:Cyclohexenes; D003692:Delayed-Action Preparations; D011108:Polymers; D012997:Solvents; D013729:Terpenes; D009568:Nitrendipine; D000077222:Limonene