Mais S. Saadallah; Omar A. Hamid
Abstract
Background: Transdermal drug delivery systems (TDDS) have been rapidly developed as a promising alternative to the oral delivery systems to provide controlled drug delivery and avoid the first-pass metabolism of drugs. Recently, various nanocarriers such as liposome and lipid nanoparticles have been ...
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Background: Transdermal drug delivery systems (TDDS) have been rapidly developed as a promising alternative to the oral delivery systems to provide controlled drug delivery and avoid the first-pass metabolism of drugs. Recently, various nanocarriers such as liposome and lipid nanoparticles have been used to enhance dermal and transdermal penetration of drugs. The aim of this study is to formulate and evaluate a polymeric nanoparticle (PNPs)-loaded transdermal patch of the antihyperlipidemic drug rosuvastatin. Materials and Methods: Rosuvastatin PNPs were prepared by nanoprecipitation method, and evaluated for particle size, zeta-potential and polydispersity index. PNPs-loaded patch and PNPs-free patch (control) of rosuvastatin were prepared by solvent casting method using hydroxyl polymethyl cellulose K15 (HPMC K 15) as film-forming polymer and polyethylene glycol 200 (PEG 200) as a plasticizer and evaluated for physical appearance, thickness, folding endurance, surface pH, in-vitro release and ex-vivo permeability. Results: The particle size, zeta-potential, and polydispersity index of rosuvastatin-loaded PNPs were 68.69 nm, - 7.5 mV, and 0.294, respectively. The prepared transdermal films showed acceptable appearance, thickness, and folding endurance as well as surface pH values. In vitro release study showed 65% and 82% cumulative release after 24 hrs for the polymeric nanoparticle-loaded patch and control patch, respectively. However. ex vivo permeation results showed that a significantly higher amount of rosuvastatin permeated via rat skin from the PNPs-loaded patch in comparison to the control patch (P-value ˂ 0.05). Conclusion: Rosuvastatin PNPs-loaded transdermal patch was successfully prepared and revealed promising releasing and permeation properties comparing to control patch.
Mais S. Saadallah; Omar A. Hamid
Abstract
Background: Transdermal drug delivery system (TDDS) is a promising delivery system that provides controlled drug release at a predetermined time. It has many advantages such as bypassing first-pass effect, increase patient convenience by providing single application rather than multiple dosing frequencies, ...
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Background: Transdermal drug delivery system (TDDS) is a promising delivery system that provides controlled drug release at a predetermined time. It has many advantages such as bypassing first-pass effect, increase patient convenience by providing single application rather than multiple dosing frequencies, and extends the action of short half-life drugs. There are three ways for drug penetration into the skin either via appendageal (shunt routes), intracellular route, and intercellular route. Permeation of drug substances through the stratum corneum remains a great challenge because it is the rate-limiting step for permeation for most molecules. Aim: This review article highlights the advances and limitations of the strategies to enhance transdermal delivery of the drugs into the skin, including both physical and chemical methods. Conclusion: The transdermal drug delivery system represents a good alternative for oral and parenteral therapy. Various penetration enhancing strategies have been successfully employed to enhance the permeation of low molecular weight molecules. For high molecular weight molecules, physical strategies such as microneedles can be used.