.

ISSN 2063-5346
For urgent queries please contact : +918130348310

TRANSFERSOMES BASED DERMAL GEL OF BACLOFEN FOR MANAGEMENT OF CHRONIC PAIN

Main Article Content

Sanjeev Kumar1, Sachin Kumar*
» doi: 10.48047/ecb/2022.12.10.593

Abstract

Baclofen's ability to relax skeletal muscles has been linked to its anti-inflammatory and stress-relieving effects. The two current baclofen treatments, oral tablets and intrathecal injection, both come with a number of undesirable systemic side effects. Developing a topical baclofen formulation to reduce the drug's systemic adverse effects was the primary goal of this research. This is accomplished by increasing the medication's penetration rate into the epidermis by increasing the time it spends in contact with the skin. The fast degradation of baclofen during first-pass metabolism accounts for its short half-life (0.4-0.8 h) and limited bioavailability (20%). This study aimed to determine the efficacy of elastic transfersome containing formulations in enhancing the skin's bioavailability of baclofen and decreasing its hepatic metabolism. It may dissolve in mild acids and bases, such as 1% acetic acid and 0.1 M NaOH. As expected, the normal melting point of 208 degrees Celsius was found to be within the range of 202 to 205 degrees Celsius. Using varied quantities of Soya-phosphatidylcholine, tween 80, span 20, and sodium deoxycholate, nine alternative formulations were developed and evaluated for particle size. The concentration of baclofen in each phase was estimated using a specific formula, and the result was used to calculate the partition coefficient. Partition coefficient data suggest that baclofen is likely to be a lipophilic compound. In order to evaluate the NPs' size and stability, we measured their particle size and zeta potential and compared the results to those of freshly made samples. Although the NPs grew in size significantly, the values of their zeta potential remained positive despite a significant decrease caused by the generation of counter charges in solution. Aggregation of NPs causes particles to grow in size, and this decrease in zeta potential may help explain why. The extrudability of gel compositions was also evaluated, with findings favouring carbopol gels.

Article Details