In-vivo study of oleic acid and tween-80 on patch transdermal A.paniculata as anti-diabetic

Abstract

Sambiloto (A.paniculata) is known empirically as a plant that could effectively treat diabetes mellitus. The substance of andrographolide in A.paniculata is able to increase insulin secretion, therefore, inhibiting alpha-glucosidase and alpha-amylase. The substances themselves have the ability to reduce blood glucose levels. Poor bioavailability due to pharmacokinetic interactions in the form of metabolism by the enzyme p-glycoprotein and CYP3A4 as well as poor physicochemical properties of water reduces bioavailability in oral administration which results in a decrease in pharmacological activity. The transdermal patch dosage form is chosen since it is considered capable of increasing the effectiveness of andrographolide in ethanol extract of sambiloto (EES). However, the challenge in transdermal preparations is the stratum corneum, which is the main barrier in transdermal drug delivery. Enhancers become a critical point in transdermal delivery. Oleic acid and tween-80 are enhancers that are widely used in transdermal patch preparations. The aim of this study was to determine the comparison of concentrations of oleic acid and tween-80 on the characteristics of transdermal patches. The transdermal patches were made using the solvent casting method with various concentration ratios of oleic acid enhancer and tween F1 (1:1), F2 (1:3), and F3 (1:2). Then, all of the formulas were tested for patch characteristics while also being tested via in-vivo antidiabetic activity using diabetic male rat. All of the formulas meet the requirements of patch characteristics. Differences in the concentration of enhancer combinations affect patch characteristics in terms of patch weight and thickness, where F2 has a greater thickness and weight than other formulas. F2 is a formula that has a greater activity than F1 and F3. F2 blood glucose level value on the fifteenth day was 105 ±2.42 mg/dL. Although subcutaneous administration of insulin is quicker in diminishing blood glucose levels, the EES F2 transdermal fix can be compelling in decreasing blood glucose levels.