DEVELOPMENT AND CHARACTERIZATION OF TRANSDERMAL DELIVERY SYSTEM OF DOXAZOSIN MESYLATE


Madhur Kulkarni, Vishakha Hastak, Supriya Jadhav

Abstract


Objective: The study involved development of transdermal delivery system (TDDS) of doxazosinmesylate (doxa) to achieve effective systemic delivery of the drug.

 

Methods: TDDS of doxa was prepared using hydroxypropyl methyl cellulose (HPMC) K100LV and polyvinyl pyrrolidone (PVP) K30 in 3:1 ratio solvent casting method.The formulation was evaluated for folding endurance, moisture uptake, pH, drug content and in vitro permeation. Various permeation enhancers were incorporated at 5% w/w concentration into the patch formulationto study their impact on the drug permeation. The TDDS made with Transcutol® as an enhancer was subjected to accelerated stability studies and in vivo skin irritation studies.

 

Results: The developed TDDS showed folding endurance of 170, moisture uptakeof 15.7%, pH  of 6.3 , drug content of 99 ± 1.1% and 66%in vitropermeation of doxaover24h. The effect of various enhancers expressed in terms of average flux can be summarized as Transcutol® (10.6 ± 2.1 µg/cm2h)> dimethyl sulfoxide(10.17± 1.2  µg /cm2h) > benzyl alcohol (9.55± 1.3  µg /cm2h) > no enhancer (8.86± 1.1  µg /cm2h)> dimethyl isosorbide (8.21± 1.5 µg /cm2h)>Isostearic acid (7.82 ± 1.4 µg /cm2h) > propylene carbonate (7.67 ± 1.4  µg /cm2h) > oleic acid (7.12 µg ± 0.8 /cm2h).  The formulation was found to be stable during the accelerated stability studies.  In vivo studies indicated absence of skin irritation effect the TDDS containing Transcutol®.

 

Conclusion: TDDS of doxacomprising HPMC K100LV and PVPK30 in the ratio of3:1 and 5% Transcutol® could serve as a potential TDDS in the treatment of benign prostatic hyperplasia (BPH) and hypertension.


Keywords


Doxazosinmesylate, transdermal patch, permeation enhancers, polyvinyl pyrrolidone, hydroxypropyl methylcellulose, Transcutol®

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