title: Transdermal delivery of lercanidipine hydrochloride: effect of chemical enhancers and ultrasound.
abstract: The effects of permeation enhancers and sonophoresis on the transdermal permeation of lercanidipine hydrochloride (LRDP) across mouse skin were investigated. Parameters including drug solubility, partition coefficient, drug degradation and drug permeation in skin were determined. Tween-20, dimethyl formamide, propylene glycol, poly ethylene glycol (5% v/v) and different concentration of ethanol were used for permeation enhancement. Low frequency ultrasound was also applied in the presence and absence of permeation enhancers to assess its effect on augmenting the permeation of drug. All the permeation enhancers, except propylene glycol, increased the transdermal permeation of LRDP. Sonophoresis significantly increased the cumulative amount of LRDP permeating through the skin in comparison to passive diffusion. A synergistic effect was noted when sonophoresis was applied in presence of permeation enhancers. The results suggest that the formulation of LRDP with an appropriate penetration enhancer may be useful in the development of a therapeutic system to deliver LRDP across the skin for a prolonged period (i.e., 24 h). The application of ultrasound in association with permeation enhancers could further serve as non-oral and non-invasive drug delivery modality for the immediate therapeutic effect.
authors.affiliation: Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, Karnataka, India. ssmutalik@yahoo.com
authors.forename: Pallavi K
authors.initials: PK
authors.lastname: Shetty
authors.forename: Neelam A
authors.initials: NA
authors.lastname: Suthar
authors.forename: Jyothsna
authors.initials: J
authors.lastname: Menon
authors.forename: Praful B
authors.initials: PB
authors.lastname: Deshpande
authors.forename: Kiran
authors.initials: K
authors.lastname: Avadhani
authors.forename: Raghavendra V
authors.initials: RV
authors.lastname: Kulkarni
authors.forename: Srinivas
authors.initials: S
authors.lastname: Mutalik
mesh_terms: D000277:Adjuvants, Pharmaceutic / Q000008:administration & dosage* / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000737:chemistry; D004095:Dihydropyridines / Q000008:administration & dosage* / Q000737:chemistry; D004126:Dimethylformamide / Q000008:administration & dosage / Q000737:chemistry; D000431:Ethanol / Q000008:administration & dosage / Q000737:chemistry; D066298:In Vitro Techniques; D051379:Mice; D010539:Permeability; D011136:Polysorbates / Q000008:administration & dosage / Q000737:chemistry; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013010:Sonication
chemical_list: D000277:Adjuvants, Pharmaceutic; D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D011136:Polysorbates; D000431:Ethanol; D004126:Dimethylformamide; C060343:lercanidipine