Objective: Domperidone Maleate is a dopamine -receptor (D 2 ) antagonist, widely used in the treatment of motion sickness and used as an antiemetic. The bioavailability of domperidone maleate when administered orally is low due to the first pass metabolism in liver, drug delivery through transdermal drug delivery has the ability to deliver the drug directly to systemic circulation by passing the liver and hence increase in bioavailability of the drug. The main aim of this investigation is to develop and evaluate matrix type transdermal drug delivery systems of domperidone maleate. Methods: The matrix type transdermal patches of Domperidone Maleate were prepared by solvent evaporation technique. The tensile strength and elongation break, in vitro drug release, in vitro drug permeation and Ex vivo permeation through rat abdominal skin were studied. The physicochemical interaction between domperidone maleate and polymer were examined by Fourier Transform Infrared Spectroscopy (FTIR). Results: All the formulations showed satisfactory physicochemical and mechanical characteristics. The optimized formulation F5 (drug: polymer ratio is 1:12.5 and 5% v/w eucalyptus oil) showed maximum cumulative percentage of drug release (1832.16±60.14 µg/ cm ) revealed that formulation F5 was strong but not brittle. FTIR studies showed no evidence of interaction between the drug and polymers. Conclusion: Domperidone maleate matrix type transdermal therapeutic systems could be prepared with the required flux and suitable mechanical properties.

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Background: Nisoldipine is an anti hypertensive drug. Nisoldipine exhibits poor oral bioavailability (5%) because of rapid metabolism in the gut and liver. To overcome hepatic first pass metabolism and to enhance bioavailability, lipid based drug delivery systems (Solid lipid nanoparticles (SLN) and nano structure lipid carriers (NLC)) can be exploited. Objectives: In this work, effort was made to prepare novel particulate carrier systems such as stable Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for transdermal delivery of Nisoldipine (NSP). For this investigation, Carbopol 934 used as gel forming agent for hydrogel preparation. Methods: Aqueous dispersions of lipid nanoparticles made from Dynasan 114, 116, 118 were prepared by hot homogenization technique followed by ultrasonication and then optimized formulations of SLN and NLCs were incorporated into the freshly prepared hydrogels. Prepared lipid nanoparticles were characterized for particle size, zeta potential, entrapment efficiency, stability and in-vitro release profile. Also percutaneous permeation of SLN and NLCs were investigated in rat abdominal skin. Results: Analyzing the particles size by photon correlation spectroscopy (PCS) using Malven zeta sizer, which shows that the SLN and NLCs were in the range of 130-330 nm at room temperature. For all the tested formulations (SLN and NLCs), the entrapment efficiency was 72-97%. In-vitro drug release studies were performed for 24 hr. In these two cases the percentage drug release from gels enriched with SLN/NLC showed sustained release over period of 24 hr. In agreement with these results NSPNLC (Nisoldipine nanostructured lipid carriers) dispersion showed faster release. Formulation E4 showed faster release has less particle size and more zeta potential. Conclusion: Based on these, it was selected for further stability and ex-vivo studies. Both the SLN and NLC showed a sustained drug release over a period of 24 hr, but the sustained effect was more pronounced with the SLN and NLC gel formulations.

Objective: Felodipine (FD) is an effective Biopharmaceutics Classification System Class II calcium channel blocker mainly used in the management of hypertension and angina pectoris. It has poor solubility and low oral bioavailability (15%). To overcome these disadvantages and to maintain constant plasma concentration for maximum therapeutic activity, there is a need to design an alternative route, that is, transdermal route. The pharmacokinetic parameters make FD a suitable candidate for transdermal delivery. The present investigation consists of the study of in vitro and ex vivo skin flux of FD from bilayered transdermal patches. Methods: The patches were fabricated by solvent casting method using hydrophilic and hydrophobic polymer with different composition. Tween 80 incorporated as solubilizer, polyethylene glycol 600 as plasticizer, menthol, eucalyptus oil, and lemongrass oil used as permeation enhancers, respectively. The prepared transdermal drug delivery system was extensively evaluated for in vitro release, ex vivo permeation through pig ear skin, moisture content, moisture absorption, water vapor transmission, and mechanical properties. The physicochemical interaction between FD and polymers was investigated by Fourier-transform infrared (FTIR) spectroscopy. Results: All the formulations exhibited satisfactory physicochemical and mechanical characteristics. A flux of 35.2 μg/cm2 h, 27.9 μg/cm2 h, and 25.25 μg/cm2 h was achieved for optimized formulations containing lemongrass oil, eucalyptus oil, and menthol, respectively, permeation enhances. Values of tensile strength (0.0652±0.034 kg/mm²) and elongation at break (0.8749±0.0.0029% mm²) revealed that formulation F9 was strong but not brittle. Drug and excipients compatibility studies showed no evidence of interaction between the active ingredient and polymers. Conclusion: Bilayered FD transdermal patches could be prepared with required flux and suitable mechanical properties.