Background: Pharmaceutical scientists are exploring the transdermal route for the treatment
of various systemic diseases nowadays. Transdermal nanocarrier systems show various advantages
like bioavailability enhancement of drugs, avoidance of first-pass hepatic metabolism, and
reduction of dosing frequency of bioactive therapeutic molecules.
Objective: The objective of the present research work was to encapsulate Propranolol hydrochloride
into oleic acid vesicles and carry out in-vitro and in-vivo evaluation of oleic acid vesicular gel containing
Methods: Propranolol hydrochloride loaded oleic acid vesicles were prepared by exploring the thin
film hydration method. Developed vesicles were evaluated for morphology, size, zeta potential and
Polydispersity Index (PDI). Thermal behavior of drug-loaded vesicles was checked using Differential
Scanning Calorimetry (DSC) and depth of skin penetration was determined using Confocal
Laser Scanning Microscopy (CLSM). Oleic acid vesicles dispersed in Carbopol 934R gel were subjected
to in-vivo evaluation in male Sprague Dawley rats through measurement of plasma concentration
and tissue distribution of Propranolol hydrochloride.
Results: Optimized formulation having oleic acid: Propranolol hydrochloride in the ratio 7 : 3
showed highest entrapment (56.1 ± 0.7%), acceptable size (291.3 ± 2.2 nm), the optimum value of
PDI (0.219 ± 0.043) and zeta potential (-27.13 ± 0.25 mV). The results of DSC analysis showed
effective encapsulation of drug inside the vesicles and CLSM analysis revealed penetration of vesicles
up to stratum spinosum layer of skin. The results of in-vivo study revealed capability of vesicular
gel to prolong the release of Propranolol hydrochloride up to 24 h with a Cmax value of 83.6 ±
3.0 ng/mL which was higher compared to the marketed tablet of Propranolol hydrochloride [Inderal
R (40 mg), Abbott India Ltd.] (45.6 ± 3.1 ng/mL). Tissue distribution studies revealed higher percentage
of Propranolol hydrochloride in various organs after 24 h of administration of vesicular gel
compared to marketed tablet.
Conclusion: Developed oleic acid vesicular gel could be effective to reduce dosing frequency and
avoid side effects of oral Propranolol hydrochloride.