Development of matrix-type transdermal delivery of lornoxicam: in vitro evaluation and pharmacodynamic and pharmacokinetic studies in albino rats.

A matrix-type transdermal drug delivery system of lornoxicam was prepared with the addition of combination of hydrophilic and hydrophobic polymers in different ratios. Transdermal patches of lornoxicam were designed with ethyl cellulose:polyvinylpyrrolidone and Eudragit RL 100:Eudragit RS 100 in different ratios with propylene glycol as plasticizer (5%) and tween 80 as permeation enhancer using the solvent evaporation technique. Evaluation of these formulations was performed through mechanical characterization and in vitro permeation studies. From the physicochemical and in vitro permeation data, the two formulations showing the best result (A3 and B3) were selected for further in vivo studies. The anti-inflammatory and analgesic effects of the patches were studied using the carrageenan paw edema model and hot plate test, respectively. The pharmacokinetic parameters were studied and recorded on animals. Formulations A3 and B3 exhibited greatest (311.04 µg and 306.32 µg, respectively) cumulative amount of drug release. The Higuchi model seemed to be the most appropriate model describing release kinetics from all patches (r(2) = 0.9847-0.9971). It was observed that both the patches significantly controlled inflammation and showed analgesic effect from the first hour (P < 0.05). Formulations A3 and B3 were found to enhance the bioavailability of lornoxicam by 3.1 and 2.7 times, respectively, with reference to the oral dosage form. Hence, lornoxicam can be formulated into transdermal patches to sustain its release characteristics and to avoid the disadvantages of oral routes. Formulations A3 and B3 were found to be the best choice to manufacture a lornoxicam transdermal drug delivery system. LAY ABSTRACT: The objective of the present work was to develop a matrix-type transdermal drug delivery system of lornoxicam with the addition of ethyl cellulose:polyvinylpyrrolidone and Eudragit RL 100:Eudragit RS 100 in different ratios with propylene glycol as plasticizer (5%) and tween 80 as permeation enhancer using the solvent evaporation technique. Lornoxicam is a non-steroidal anti-inflammatory drug that is used for the treatment of pain, inflammation, and arthritis. The prepared patches were evaluated for mechanical characterization and in vitro permeation studies. The formulations showing best results (A3 and B3) were selected further for in vivo and pharmacokinetic studies on animals. From the results, it was found that formulations A3 and B3 exhibited greatest cumulative amount of drug release, controlled inflammation, and showed analgesic effect from the first hour. Hence, lornoxicam can be formulated into transdermal patches, and formulations A3 and B3 were found to be the best choice to manufacture a lornoxicam transdermal drug delivery system.

Design and evaluation of patches for transdermal delivery of losartan potassium.

The present work comprises the formulation and evaluation of losartan potassium with a view to developing and preparing a losartan potassium releasing system for transdermal applications. The aim of the study was to prepare the transdermal patch of drug using different blends of polymers. Transdermal patches of losartan potassium were prepared using ethyl cellulose (EC): polyvinyl pyrrolidone (PVP), Eudragit RL-100: Eudragit RS-100 and polyvinyl alcohol (PVA): polyvinyl pyrrolidone (PVP) using different ratios by the solvent casting technique. Physicochemical parameters like flexibility, thickness, smoothness, moisture content, hardness, and tensile strength were studied. The in vitro permeation study was carried out using a modified Keshery diffusion cell, and the formulation followed the Higuchi diffusion mechanism. The blood pressure lowering response of all formulations was studied using hypertension-induced rats by the chronic renal hypertension method. The formulation containing Eudragit RL-100: Eudragit RS-100 as polymers showed satisfactory drug release pattern (hydrophobic polymers) compared to combination of hydrophobic and hydrophilic polymers (EC: PVP) and PVA: PVP (hydrophilic polymers). The amount of drug release from formulations containing hydrophilic polymers and combination of both hydrophobic and hydrophilic polymers were found to be less in comparison to the patches of hydrophobic polymers. LAY ABSTRACT: The aim of the present study was to prepare and evaluate the transdermal patch of drug using different polymers such as hydrophobic, combination of hydrophobic: hydrophilic, and hydrophilic. Losartan potassium (hydrophilic) is the antihypertensive drug used for lowering increased blood pressure. Transdermal patches of losartan potassium were prepared using different ratios of polymers by the solvent casting technique. The prepared patches were evaluated for their flexibility, thickness, smoothness, moisture content, hardness, and tensile strength. The in vitro permeation study was carried out using a diffusion cell. The blood lowering response of all formulations was studied using hypertension-induced rats. The formulation containing hydrophobic polymers showed a satisfactory drug release pattern compared to the combination of hydrophobic: hydrophilic polymers and the hydrophilic polymers. Hence, the present study reveals that formulation of hydrophilic drug (losartan potassium) withhydrophobic polymers exhibit good release properties as compared to that of hydrophilic polymers and combination of both hydrophobic and hydrophilic polymers.