Formulation and Evaluation of Nanostructured Lipid Carrier (NLC)–based Gel of Valdecoxib (original) (raw)
Related papers
The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon 90G as the co-surfactant were used. NLCs were prepared by melt-emulsification, low-temperature solidification, and high-speed homogenization methods. Characterization of the NLC dispersion was carried out through particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and an in vitro release study. The anti-inflammatory effect of the NLC gel was assessed by the rat paw edema technique and compared to marketed aceclofenac gel. The NLC dispersions exhibited d90% between 233 nm and 286 nm. All of the NLC showed high entrapment efficiency ranging from 67% to 82%. The particle size of NLC was further confirmed by the SEM study. The result of DSC showed that aceclofenac was dispersed in NLC in an amorphous state. Both the entrapment and release rate were affected by the percentage of oleic acid, but the method of preparation affected only the entrapment efficiency. The nanoparticulate dispersion was suitably gelled and assessed for in vitro permeation. Finally, NLC-based gels were found to possess superior (almost double) the anti-inflammatory activity compared to the marketed product. The anti-inflammatory activity of NLC gel showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel.
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.
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.
Transdermal delivery of drugs through the skin to systemic circulation provides a convenient 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 delivery and iontophoretic delivery. Iontophoresis for 10 minutes was carried out in combination with penetration enhancers as well as without penetration enhancers. Iontophoretic delivery of optimized formulation (F3) which has chemical penetration enhancers (2% tween 80) showed higher anti-inflammatory activity (73%) as compared to passive delivery of F1 (22%) and in chemical method of delivery of F3 (40%) in 1 to 4 hours. So, delivery of Lornoxicam is affected by various methods of permeation enhancement in which combination of physical and chemical methods seems to be much effective. 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.
FORMULATION AND EVALUATION OF TRANSDERMAL DRUG DELIVERY SYSTEM CONTAINING ANTI-INFLAMMATORY AGENT.
Aim of the present study was to develop site-specific drug delivery system of lornoxicam for the treatment of arthritis, pain etc., which has excellent activity on inhibition of Cyclooxygenase-1 and Cyclooxygenase-2 enzymes. The formulations were developed by utilizing variouspolymers such as hydroxy propyl methyl cellulose and Eudragit RL-100 by solvent casting technique by the use of plasticizer (PEG-400 & DBT). The calibration curve of lornoxicam was developed in methanol/water. Compatibility study was carried out by FT-IR and Differential scanning colorimetry. The formulations were evaluated for thickness, folding endurance, weight variation, drug content, percent moisture loss, tensile strength. In vitro drug release study was also carried out by using PBS pH 7.4 and the samples were analyzed UV-spectrophotometrically at 374 nm. FT-IR and DSC study revealed no interaction between drug and polymers. Formulations shown good uniformity of drug content, there was no any kind of effect on moisture loss test. Formulations showed thickness within the range of (0.072 to 0.119). Formulation F1, F2, F5 & F6 showed good tensile strength. By increasing the concentration of Eudragit RL-100 in the formulation tensile strength, and folding endurance increases. Formulation F6 shows the release of drug 96.74% at the end of 12 h and was considered as a best formulation. A short‐term stability study of the optimized formulation (F6) was also carried out at 400C for three months. At periodic interval 0, 30, 60, and 90 days a known quantity of sample was withdrawn and then analyzed for drug content and in vitro drug release studies, results showed a good content of uniformity and 95.23% release was observed at the end of 90 days. After a short-term stability study, there was no or very little amount of degradation was observed.
Journal of Pharmacy Research, 2013
Aims: The work is aimed to formulate aqueous nanodispersion of aceclofenac Nanostructured Lipid Carriers (NLC) by using modified hot sonication method and to prepare NLC based gel for topical delivery of aceclofenac. Methods: The lipids incorporated in the study were Compritol 888 ATO and Miglyol and the emulsifier/stabilizer used was Polysorbate 80. The formulations were optimized by using 3 factor, 3 levels, BoxeBehenken design. The independent variables were combination of lipids (% w/w), concentration of emulsifier (% w/v), lipid drug ratio and the response variables were particle size, percentage entrapment and drug release after 12 h. The formulations were also characterized for particle size, entrapment efficiency, drug loading and depression in melting point. Results: The DSC, FTIR analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by SEM which showed spherical shape of the formulations. Further the formulations were evaluated for in vitro drug permeability study, rheological properties, skin irritation, pharmacodynamic and stability studies. Conclusion: The pharmacodynamic characteristics of aceclofenac NLC gel with reference to the conventional gel were compared by using Carrageenan induced rat paw edema method. The study showed the promising and stable alternative form for the aceclofenac for topical application.
Design and optimization of lomefloxacin loaded NLC gel for ophthalmic drug delivery
International Journal of Health Sciences (IJHS), 2022
Lomefloxacin is a fluoroquinolone drug that has broadspectrum action against Gram-negative as well as Gram Positive pathogens. The drug retention issues of ophthalmic drug delivery are a key parameter to select NLC gel as a deliver system. The purpose of the present investigation was to design, optimize and evaluate Lomefloxacin loaded nano structured lipid gel for Ophthalmic Drug Delivery. Lomefloxacin loaded NLCs were prepared by high-pressure homogenization approach (hot), using Olive oil as liquid lipid, Stearic acid as solid lipid and tween 80 as surfactant. Box-Behnken design was used to optimize Lomefloxacin loaded NLCs using Design-Expert 12 programme. Lipid ratio X1, surfactant concentrationX2, and homogenization cycle X3 are kept as three independent variables particle size (Y1 nm), entrapment efficiency (Y2 percent), and drug release percentage (Y3 percent) as dependent variables. NLCs were characterized for particle size, zeta potential and entrapment efficiency. The effects of composition of lipid materials and surfactant mixture on the particle size, zeta potential, drug entrapment efficiency, and in vitro drug release behavior were investigated. The formulation composed of 8 mg of lipid, 3.19 ml of surfactant, and a homogenization cycle of 2 cycles resulted in the optimal formulation as it has shown a particle size, entrapment efficiency, and drug release percentage within projected limits, at 209.243nm, 81.74 percent, and 89.76 percent, respectively.
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.
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.