Evaluating Transdermal Delivery of Labetalol Hydrochloride: Role of Penetration Enhancers
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Abstract
Transdermal drug delivery has gained attention as a viable alternative to traditional oral and parenteral routes, especially for drugs with significant first-pass metabolism such as labetalol hydrochloride. This study investigates the feasibility of delivering labetalol hydrochloride through the transdermal route and examines the impact of various chemical penetration enhancers on its skin permeability. Labetalol hydrochloride, a widely used antihypertensive agent, suffers from reduced oral bioavailability, making controlled transdermal administration a potential strategy to maintain therapeutic plasma concentrations with improved patient compliance. In this research, in vitro permeation studies were conducted using excised rat skin in Franz diffusion cells. Penetration enhancers such as ethanol, propylene glycol, oleic acid, and dimethyl sulfoxide (DMSO) were incorporated into the drug formulation to assess their effect on transdermal flux. The cumulative drug permeation and enhancement ratios were calculated to evaluate efficacy. Results demonstrated a significant increase in permeability with selected enhancers, particularly oleic acid and DMSO, without causing notable skin irritation. The findings suggest that transdermal delivery of labetalol hydrochloride is feasible and can be significantly improved with appropriate penetration enhancers. This approach may provide a more effective and patient-friendly alternative for long-term hypertension management.
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