Comparative release profiles of Benzoyl Peroxide from different pharmaceutical dosage forms

ME ACEVEDO; A. FERNANDEZ; C. SALERNO; V. MOURIÑO

Jornada; 4ta Reunión Internacional de Ciencias Farmacéuticas (RICIFA 2016); 2016

UNIVERSIDAD DE ROSARIO

Acne is a multifactorial pathology since several processes are involved in its development: increased sebum production, keratinization, P. acnes proliferation and inflammation. The treatment depends on the clinical stage and topical therapy is of choice in mild to severe inflammatory acne1,2. Benzoyl Peroxide (BPO) is a first line drug for topical treatment because of its benefits respect to other antibiotics and keratolytics since BPO combines antimicrobial and keratolytic activity without bacterial resistant reported so far3. BPO effect is dose dependant however irritation increases with concentration so dosage forms for a slow and constant release of drug would be advantageous4. The aim of this work was to evaluate and compare in vitro drug release from different semisolids matrixes for PBO. For this purpose a commercial emulgel formula (Vixiderm E® Gel, ICN), a conventional Carbomer® 940 gel and a lipogel with Octyldodecanol were compared; all the formulations had BPO 5%. The study was performed according to Guidance for Industry Nonsterile Semisolid Dosage Forms 5. Franz cells were used with polysulfone membranes and water:acetone 50:50 as receptor media. Sampling was made at 0.5, 1, 2, 4 and 6 h. Drug quantification was made by HPLC, column Lichopher RP-18 (5µm) and UV detection at 254 nm. All quantitative results were obtained from assays using three samples. Data was expressed as the mean ± standard deviation (SD). Student?s t-test was used for statistical analysis. A value of p < 0.05 was considered to be statistically significant. ANOVA was used for comparing data from studies.The amount of BPO released from the different semisolid formulations (Vixiderm E®, conventional gel and lipogel) studies increased along the study, and the cumulative BPO released by the end of the study was 31.3±3.1%, 22.9±1.9%, 24.8±1.8%, respectively. The drug release from Vixiderm® was significantly higher than the other tested formulations (p˂0.05). Particularly, during the first hour of study, the amount of BPO released from lipogel showed no significant difference than that of BPO released from Vixiderm E® (14.7±1.1% and 12±1.3%, respectively); in contrast, the amount of BPO released from conventional gel was significantly lower (8.6±0.6%; p˂0.05). Further, the release profile of BPO from lipogel showed a steady increase in each time frame indicating controlled and sustained release profile. The greater initial release of BPO from Vixiderm E® and lipogel could be due to increased BPO solubility in both formulations (in contrast to what was released from the Carbomer® gel), but the crystalline structure of the lipogel favored the slow release.