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Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride.

Prasanthi D, Lakshmi PK - ISRN Pharm (2012)

Bottom Line: All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug.Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr.Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Andhra Pradesh 500 028, India.

ABSTRACT
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.

No MeSH data available.


Related in: MedlinePlus

Release profile of formulations CA1 to CA8 in comparison to control through dialysis membrane.
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Related In: Results  -  Collection


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fig1: Release profile of formulations CA1 to CA8 in comparison to control through dialysis membrane.

Mentions: The diffusion studies were performed on locally fabricated keshary-chein diffusion cell through dialysis membrane. The percentage release in 24 hrs by different enhancers when compared with control is shown in Figures 1 and 2. The release rate of these formulations is given in Table 3. Formulation CA9 containing tween-20 (1%) showed the maximum release (396.36 ± 0.53 μg/cm2/hr1/2) in 6 hrs only, and CA13 formulation containing dimethyl sulfoxide 5% showed the maximum release (324.07 ± 0.52 μg/cm2/hr1/2) in 12 hrs only. Formulations CA3 and CA4 containing oleic acid 2.5% and 5%, respectively, decreased release (58.95 ± 0.39 μg/cm2/hr1/2, 20.81 ± 0.28 μg/cm2/hr1/2) of drug when compared to control. Each enhancer was formulated in two different concentrations, and with an increase in concentration, increase in release rate was observed except with oleic acid, tween-20, and dimethyl sulfoxide where release rate was decreased with increase in concentration.


Effect of chemical enhancers in transdermal permeation of alfuzosin hydrochloride.

Prasanthi D, Lakshmi PK - ISRN Pharm (2012)

Release profile of formulations CA1 to CA8 in comparison to control through dialysis membrane.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3539352&req=5

fig1: Release profile of formulations CA1 to CA8 in comparison to control through dialysis membrane.
Mentions: The diffusion studies were performed on locally fabricated keshary-chein diffusion cell through dialysis membrane. The percentage release in 24 hrs by different enhancers when compared with control is shown in Figures 1 and 2. The release rate of these formulations is given in Table 3. Formulation CA9 containing tween-20 (1%) showed the maximum release (396.36 ± 0.53 μg/cm2/hr1/2) in 6 hrs only, and CA13 formulation containing dimethyl sulfoxide 5% showed the maximum release (324.07 ± 0.52 μg/cm2/hr1/2) in 12 hrs only. Formulations CA3 and CA4 containing oleic acid 2.5% and 5%, respectively, decreased release (58.95 ± 0.39 μg/cm2/hr1/2, 20.81 ± 0.28 μg/cm2/hr1/2) of drug when compared to control. Each enhancer was formulated in two different concentrations, and with an increase in concentration, increase in release rate was observed except with oleic acid, tween-20, and dimethyl sulfoxide where release rate was decreased with increase in concentration.

Bottom Line: All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug.Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr.Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, G. Pulla Reddy College of Pharmacy, Osmania University, Hyderabad, Andhra Pradesh 500 028, India.

ABSTRACT
The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q(24)) of 702.28 ± 6.97 μg/cm(2) and 702.74 ± 7.49 μg/cm(2), respectively. A flux rate of 31.08 ± 0.21 μg/cm(2)/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm(2)/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH.

No MeSH data available.


Related in: MedlinePlus