In Vitro Permeation Studies on Carvedilol Containing Dissolving Microarray Patches Quantified Using a Rapid and...

Area of Science:

• Pharmaceutical Analysis
• Drug Delivery Systems
• Analytical Chemistry

Background:

• Analytical method validation is crucial for drug formulation and delivery research.
• Quantifying carvedilol (CAR) requires sensitive and reliable analytical techniques.
• Previous methods may lack the efficiency or sensitivity needed for complex matrices like biological tissues.

Purpose of the Study:

• To develop and validate a high-performance liquid chromatography with UV detection (HPLC-UV) method for quantifying carvedilol (CAR).
• To establish an efficient extraction procedure for CAR from excised neonatal porcine skin.
• To apply the validated method to assess CAR permeation through skin using a dissolving microarray patch (MAP).

Main Methods:

• Isocratic elution using a C18 column with a mobile phase of 0.1% trifluoroacetic acid in water and acetonitrile (65:35 v/v) at 0.6 mL/min.
• Method validation followed International Council on Harmonization (ICH) guidelines, assessing linearity, specificity, accuracy, precision, and robustness.
• Extraction of CAR from neonatal porcine skin samples followed by quantification using the developed HPLC-UV method.

Main Results:

• The HPLC-UV method demonstrated excellent linearity for CAR in phosphate-buffered saline (1.5-50 μg/mL, R²=0.999) and methanol (0.2-6.2 μg/mL, R²=0.9999).
• The method proved to be specific, accurate, precise, and robust, meeting ICH requirements.
• Extraction recovery rates for CAR from neonatal porcine skin ranged from 95% to 97%.

Conclusions:

• A validated, sensitive, and robust HPLC-UV method was successfully developed for CAR quantification.
• An efficient extraction technique for CAR from porcine skin was established.
• The validated method and extraction procedure were effectively applied to evaluate CAR permeation from a dissolving MAP in transdermal and intradermal studies.