FORMULATION AND EVALUATION OF TRANSDERMAL GEL OF LORNOXICAM AND COMPARITIVE DIFFUSION STUDY BY IONTOPHORESIS AND CHEMICAL ENHANCERS (original) (raw)
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FORMULATIONAND EVALUATION OF TRANSDERMAL GEL OF LORNOXICAM IN COMBINATION WITH CHEMICAL ENHANCERS
ABSTRACT Transdermal delivery of drugs through the skin to systemic circulation provides aconvenient route of administration for a variety of clinical indications. The purpose of present investigation was to develop Lornoxicam transdermal gel and its iontophoretic delivery to enhance its permeation for systemic effect and to avoid side effects and minimize frequency of administration. Lornoxicam (NSAIDs) is a COX-1 and COX-2 inhibitor used in the treatment of inflammation, pain and edema, rheumatoid arthritis and so on. Transdermal gel of Lornoxicam was formulated using triethanolamine (5%) as solvent, carbopol 934p as gelling polymer and various penetration enhancers and enhancement in its permeation by using chemical enhancers and iontophoresis was investigated. Formulated gel was evaluated with respect to different physiochemical parameters such as pH, viscosity, spreadability, gel strength. Permeation study was carried out using cellophane membrane and phosphate buffer pH 6.8 for 6 hours. Anti- inflammatory activity of Lornoxicam gel was studied in albino rats by carrageenan induced paw edema method in which Lornoxicam gel was delivered through rat’s skin by passive diffusion and diffusion with chemical enhancers. Optimized formulation (F3) with chemical penetration enhancers (tween 80, 2%) showed higher anti-inflammatory activity (40 %) as compared to F1 (22%) in 1 to 4 hours. So, diffusion of Lornoxicam is affected by presence of chemical enhancers.Stability studies carried out at different temperatures and humidity did not show any significant change in drug content, % CDR, viscosities and other parameters at the end of 12 weeks indicating that all the formulations were stable. Physiochemiclly stable and non-irritant Lornoxicam gel was formulated which could deliver significant amount of active substances across the skin in-vitro and in-vivo which elicit the anti-inflammatory activity. Keywords: Lornoxicam, penetration enhancers, NSAID’s, tween 80, anti-inflammatory activity.
Development and Evaluation of Transdermal Gel of Lornoxicam
Universal Journal of Pharmaceutical Research, 2017
Transdermal drug delivery systems deliver the drug through the skin at controlled rate to the systemic circulation. It mainta ins the blood concentration of the drug within the therapeutic system window ensuring that drug levels neither fall below the minimum effective concentration nor exceed the minimum toxic dose. The objective of the present work was to formulate transdermal gel of Lornoxicam. It is a COX-1 and COX-2 inhibitor used in the treatment of inflammation, pain and edema, rheumatoid arthritis. Transdermal gel of Lornoxicam was formulated using triethanolamine as solvent, HPMC K100 and EC as polymers. Formulated gel was evaluated with respect to different physiochemical parameters such as pH, viscosity, spreadability. In-vitro release study was performed for 10 hrs. Selected formulation was subjected to stability testing at different temperatures.
2014
Objective: The objectives of present investigation were to develop transdermal system for Lornoxicam using chitosan as rate controlling polymer and Tween 20 as permeation enhancer. Then evaluate the effect of Tween 20 on the physico-chemical properties of the patches and on drug permeation across the membrane. Methods: Transdermal patches of Lornoxicam were prepared by solvent casting method. The prepared patches were evaluated for physicochemical characteristics such as in vitro drug release, skin irritation studies. The interaction between drug and polymer were investigated by FTIR, DSC, XRPD methods. Results: The in vitro release studies revealed Formulation L4 containing higher concentration of Tween 20 showed 74.6% diffusion in 12 h and follows Korsmeyer-Peppas drug release kinetics. Respective formulation did not showed any sign of erythema or edema in skin irritation test. FTIR study reveals good compatibility between drug and polymer. Conclusion: The prepared transdermal drug delivery system of Lornoxicam using Chitosan had shown good promising results for sustained release matrix transdermal patch formulation.
PLOS ONE
The aim of the current study was to develop membrane-based transdermal patches of lornoxicam gel using oleic acid (OA)and propylene glycol (PG) as penetration enhancers to improve drug delivery across the skin and to evaluate in vivo analgesic and anti-inflammatory activity. For this purpose, nine formulations were developed in accordance with 3 2 factorial design using Design Expert ® 11. The concentration of propylene glycol (X 1) and oleic acid (X 2) were selected as independent variable whereas Q 10 (Y 1), flux (Y 2) and lag time (Y 3) were considered as the response variables. The impact of drug loading, surface area, gel concentration, membrane variation and agitation speed on drug release and permeation was also studied. The skin sensitivity reaction, analgesic activity and anti-inflammatory action of the optimized patch were also determined in Albino Wistar rats. Stability studies were performed for three months at three different temperature conditions. The result suggests that a membrane-based system with controlled zero-order drug release of 95.8 ± 1.121% for 10 h exhibiting flux of 126.51±1.19 μg/cm 2 /h and lag time of 0.908 ±0.57h was optimized with the desired analgesic and anti-inflammatory effect can be obtained by using propylene glycol and oleic acid co-solvents as a penetration enhancer. The patch was also found stable at 4˚C for a period of 6.44 months. Formulation F9 comprising of 10% PG and 3% OA was selected as an optimized formulation. The study demonstrates that the fabricated transdermal system of lornoxicam can deliver the drug through the skin in a controlled manner with desired analgesic and anti-inflammatory activity and can be considered as a suitable alternative of the oral route.
The purpose of this work is to develop and evaluate matrix-type transdermal patch containing drug Lornoxicam with different ratios of hydrophilic (PVA) and hydrophobic (Ethyl cellulose) polymeric systems, in which 4 % w/v of Tween 80 as penetration enhancer and 10 % w/v of PEG 400 as plasticizer in dichloromethane and methanol (4:1) solvent system by using Solvent Evaporation Technique. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, tensile strength, folding endurance, percentage moisture loss, percentage moisture uptake, and water vapour transmission rate. Drug excipients compatibility studies are confirmed by using FTIR Spectrums. In-vitro permeation studies of formulations were prepared by using Franz diffusion cells. Mechanism of drug release was determined by Korsmeyer-Peppas equation. The 'n' values were found in the range of 0.836-1.159. It indicated that the formulation follows diffusion mechanisms of both non-Fickian and super case II transport. The kinetic studies showed that, formulation F-1 follow zero order while formulations F-2 to F-7 follow fist order. These results indicate that the formulation F3 {poly vinyl alcohol: Ethyl cellulose (1:1)} has shown optimum release of 79.34% with its action sustained for 24 hours time period.
The Scientific World Journal, 2014
The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also, in vitro skin permeation of LOR was conducted. The effect of hydroxypropyl -cyclodextrin (HP -CD), beta-cyclodextrin ( -CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 g/cm 2 /h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HP -CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HP -CD and may be promising in enhancing permeation.
Indian Journal of Pharmaceutical Education and Research, 2019
Objective: The objectives of present investigation were to develop transdermal system for Lornoxicam using chitosan as rate controlling polymer and Tween 20 as permeation enhancer. Then evaluate the effect of Tween 20 on the physico-chemical properties of the patches and on drug permeation across the membrane. Methods: Transdermal patches of Lornoxicam were prepared by solvent casting method. The prepared patches were evaluated for physicochemical characteristics such as in vitro drug release, skin irritation studies. The interaction between drug and polymer were investigated by FTIR, DSC, XRPD methods. Results: The in vitro release studies revealed Formulation L4 containing higher concentration of Tween 20 showed 74.6% diffusion in 12 h and follows Korsmeyer-Peppas drug release kinetics. Respective formulation did not showed any sign of erythema or edema in skin irritation test. FTIR study reveals good compatibility between drug and polymer. Conclusion: The prepared transdermal drug delivery system of Lornoxicam using Chitosan had shown good promising results for sustained release matrix transdermal patch formulation.
Iraqi Journal of Industrial Research, 2023
Lornoxicam was practically water insoluble and a nonsteroidal antiinflammatory therapeutic agent thus associated with gastrointestinal tract (GIT) side effects. Lipid polymer hybrid nanocarriers (LPHNs)based transdermal nanogel of lornoxicam was formulated to increase solubility of lornoxicam and sustained lornoxicam release that lead to eliminate GIT related side effect, prolong therapeutic activity and improve patient compliance .The lornoxicam LPHNs formulations (LH1-LH6) were prepared by microwaves based method. The conventional gel of lornoxicam (G) was prepared by solvent diffusion method. The LH1-LH6 was entered to characterization processes that were later used as a base to prepare lornoxicam hybrid nanogel formulations (LN1-LN6). The LN1-LN6 was tested for various evaluations. It was found that all the LH1-LH6 were show nanosize globules, low polydispersity index and acceptable surface charge, entrapment efficiency and drug loading. LH3 was the most optimized LPHNs due had lower particle size and higher lornoxicam release.The evaluation processes indicate stable organoleptic properties, high homogeneity, and acceptable values of pH. The comparability profile of the lornoxicam release from the lornoxicam nanogel formulations (LN1-LN6) and conventional lornoxicam gel (G) was in the following descending order: LN3 > LN2> LN1 > LN6 > LN5 > LN4 > G. The characterization and evaluation processes highly support promise transdermal delivery system to decrease pain and inflammation in musculoskeletal diseases.
The gastric irritant effects of peroral lornoxicam can be attenuated using skin as the route of administration. The present work was focused on the development, characterization, ex vivo skin permeation and skin targeting behaviors of lornoxicam-loaded solid lipid nanoparticles (SLN). Lornoxicam loaded SLN was prepared by emulsification solvent evaporation technique. The particle size and polydispersity index were measured by dynamic light scattering technique and was found to be at 180.7±4.4 nm, 0.223±0.006, respectively. The shape and surface topography of SLN were observed by transmission electron microscopy (TEM). Lornoxicam loaded SLN gel and lornoxicam gels were prepared and the gels were evaluated with respect to in vitro occlusivity, skin irritation and ex vivo skin permeation studies. Lesser skin irritancy and good oclusivity was observed with SLN gel as compared to the lornoxicam gel formulation. The ex vivo permeation data showed that SLN gel could significantly increase the extent of lornoxicam in skin and it showed skin targeting effect significantly. The anti-inflammatory activity of lornoxicam loaded SLN gel was stronger than that of lornoxicam gel and marketed formulation in carrageenan induced rat paw edema. These results suggest the SLN gel as the promising carrier for topical delivery of lornoxicam with skin targeting potential.
Gelatin-based nanoparticles as drug delivery system of lornoxicam gel
2016
The purpose of contemporary study was to project GNP by using of two step desolvation method. Biodegradable hydrophilic gelatin nanoparticles used as a delivery system of anti-inflammatory lornoxicam after gel formulation using each of hydroxyl propyl methyl cellulose (HPMC) and carbopol as gelling agent. The size and shape of the nanoparticles were examined by optical microscope and transmission electron microscopy, particles with a mean diameter of 240.6 nm and 0.1 poly dispersibility index PDI were produced and the percentage of entrapment efficiency was found to be 87.1%. The optimum amount of LOR loading was obtained. Four formulas were prepared F1, F2 are slandered drug gel and F3 and F4 are GNP-LOR gel. Permeation of drug through membrane was determined by Franz diffusion cell. Further stability studies were carried out at 4°C for a period of 8 weeks. Vivo study was carried on white albino male rats to compare between different lornoxicam gel formulations. Results show that the two step desolvation is an appropriate method for preparing GNP as a delivery vehicle for LOR gel which gives sustained drug release. LORF3 which has carbopol as gelling agent was of lower release rate as regard carbopol was found to be a good choice for formulating LOR as topical formulation.