PREPARATION AND IN-VITRO STUDIES OF 17-Β-ESTRADIOL AND LEVONORGESTREL TRANSDERMAL PATCHES USING NOVEL TRANSDERMAL PERMEATION ENHANCERS

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DAVARAN S.; RASHIDI M.R.; JAVADI M.; HAMISHEHKAR H.

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Journal: PHARMACEUTICAL SCIENCES Year:2006 | Volume:- | Issue:3 Page(s): 25-32

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Title

PREPARATION AND IN-VITRO STUDIES OF 17-Β-ESTRADIOL AND LEVONORGESTREL TRANSDERMAL PATCHES USING NOVEL TRANSDERMAL PERMEATION ENHANCERS

Author(s)

DAVARAN S. | RASHIDI M.R. | JAVADI M. | HAMISHEHKAR H. | Issue Writer Certificate

Keywords

17-Β-ESTRADIOLQ2

LEVONORGESTRELQ2

CONTRACEPTIVE PATCHQ2

POLYETHYLENE GLYCOL CITRATEQ2

PERMEATION ENHANCEQ2

Abstract

Objectives: There is considerable interest in the skin as a site of drug application both for local and systemic effect. However, the skin, in particular the stratum corneum, poses a formidable barrier to drug penetration thereby limiting topical and transdermal bioavailability. Skin penetration enhancement techniques have been developed to improve bioavailability and increase the range of drug for which topical and transdermal delivery is a viable option. Methods: Contraceptive drug-in-adhesive patches containing 17-Β-ESTRADIOL and LEVONORGESTREL were prepared using the acrylic type pressure sensitive adhesive (PSAs, DUROTAK2287) and the mixture of poly ethylene glycol citrate (PEG-CA), ethyl lactate (EL) and dimethyl sulfoxide (DMSO) as the chemical skin PERMEATION ENHANCErs. The enhancing effects of various enhancers with different concentrations on the permeation of 17-Β-ESTRADIOL and LEVONORGESTREL were evaluated using Frantz diffusion cells fitted with rat skin. Results: The results showed that at the highest concentration of enhancers (2%) the rank order of enhancement effect for both drugs was PEG-CA/EL/DMSO 3/1/1 mixture> PEG-CA>EL>DMSO. In the presence of PEG-CA/EL/DMSO 3/1/1 mixture, the steady state flux for 17-β- estradiol and LEVONORGESTREL were 0.455 ± 0.043μgcm-2h-1 and 1.416 ± 0.132 μgcm-2h-1respectively. It was also shown that increasing the concentration of enhancer mixture led to reduction in the adhesion property of the PSAs. Conclusion: Dosage units were provided which transdermally deliver at least minimum daily doses of 17-Β-ESTRADIOL and LEVONORGESTREL for multiple days, such as for one week.

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APA: Copy

DAVARAN, S., RASHIDI, M.R., JAVADI, M., & HAMISHEHKAR, H.. (2006). PREPARATION AND IN-VITRO STUDIES OF 17-Β-ESTRADIOL AND LEVONORGESTREL TRANSDERMAL PATCHES USING NOVEL TRANSDERMAL PERMEATION ENHANCERS. PHARMACEUTICAL SCIENCES, -(3), 25-32. SID. https://sid.ir/paper/48523/en

Vancouver: Copy

DAVARAN S., RASHIDI M.R., JAVADI M., HAMISHEHKAR H.. PREPARATION AND IN-VITRO STUDIES OF 17-Β-ESTRADIOL AND LEVONORGESTREL TRANSDERMAL PATCHES USING NOVEL TRANSDERMAL PERMEATION ENHANCERS. PHARMACEUTICAL SCIENCES[Internet]. 2006;-(3):25-32. Available from: https://sid.ir/paper/48523/en

IEEE: Copy

S. DAVARAN, M.R. RASHIDI, M. JAVADI, and H. HAMISHEHKAR, “PREPARATION AND IN-VITRO STUDIES OF 17-Β-ESTRADIOL AND LEVONORGESTREL TRANSDERMAL PATCHES USING NOVEL TRANSDERMAL PERMEATION ENHANCERS,” PHARMACEUTICAL SCIENCES, vol. -, no. 3, pp. 25–32, 2006, [Online]. Available: https://sid.ir/paper/48523/en

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