scholarly journals Formulation and Evaluation of Lecithin Organogel for Treatment of Arthritis

2015 ◽  
Vol 1 (7) ◽  
pp. 300
Author(s):  
MAHENDRA PRASAD JATAV
Keyword(s):  
Skin Irritation ◽  
In Vitro Release ◽  
Joint Stiffness ◽  
Topical Administration ◽  
Daily Basis ◽  
In Vivo Evaluation ◽  
Gastrointestinal Complications ◽  
Increased Risk

AbstractArthritis is a disease of the joint that involves inflammation of one or more joints. The common symptoms of arthritis disorders include varied levels of pain, swelling, joint stiffness, and sometimes a constant ache around the joints. More than 20 million individuals with arthritis have severe limitations in function on a daily basis. The objective of this study was to resolve conventional dosage forms of NSAIDs, which are at increased risk for serious gastrointestinal complications, when administered through oral route. Topical administration of NSAIDs could deliver lornoxicam to the site of action in rheumatic diseases which would reduce the gastrointestinal complications and side effects of the drug. The prepared organogel of lornoxicam were evaluated for its appearance, organoleptic characteristic, viscosity, gelation temperature, drug content and in vitro release study. In vivo evaluation for analgesic activity of formulation was carried out in terms of skin irritation study, hot plate method, writhing test and edema paw induce method.Keywords- Lornoxicam, lecithin, organogel, Arthritis, Topical delivery.

scholarly journals Formulation and evaluation of lecithin organogel for treatment of arthritis

2015 ◽  
Vol 3 (2) ◽  
pp. 267 ◽  
Author(s):  
Mahendra Prasad Jatav ◽  
Suman Ramteke
Keyword(s):  
Aqueous Phase ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Topical Administration ◽  
Isopropyl Myristate ◽  
In Vivo Evaluation ◽  
Gastrointestinal Complications ◽  
Drug Content

<p><strong>Background:</strong> Arthritis is a disease of the joint that involves inflammation of one or more joints. Topical administration of NSAIDs could deliver lornoxicam to the site of action in rheumatic diseases, which would reduce the gastrointestinal complications and side effects of the drug.</p><p><strong>Methods:</strong> In this method, the oily phase was prepared by dispersing the specific amount (ratio; 40:60) of purified lecithin at room temperature in isopropyl myristate as dispersing and emulsifying agent. The aqueous phase of polypropylene was prepared by dispersing a weighed amount of polypropylene and glycerol in water. It was stored at 2-4 oC overnight for the effective dissolution. The aqueous phase was slowly added in oily phase with stirring at 400 rpm using a mechanical stirrer. The prepared organogel of lornoxicam were evaluated for its appearance, organoleptic characteristic, viscosity, gelation temperature, drug content and in vitro release study. In vivo evaluation for analgesic activity of formulation was carried out in terms of skin irritation study, hot plate method; writhing test and edema paw induce method.</p><p><strong>Results:</strong> The drug content of organogel formulations was found in the range of 92.43±2.10-97.93±0.31% indicating uniform distribution of drug through the base and no interaction of drug with component of base. Posthoc Dunnet’s t-test by employing statistical software, GraphPad InStat 3. It’s shown differences between groups were considered significant at P &lt; 0.05.</p><p><strong>Conclusion:</strong> The transdermal organogel formulation of lornoxicam could provide significant anti-inflammatory and antirheumatic activity when applied topically and was observed to be functional for topical delivery of lornoxicam.</p>

Improved percutaneous delivery of azelaic acid employing microemulsion as nanocarrier: formulation optimization, in vitro and in vivo evaluation

RSC Advances ◽  
2015 ◽  
Vol 5 (37) ◽  
pp. 28985-28995 ◽  
Author(s):  
Huixian Ma ◽  
Meng Yu ◽  
Fengping Tan ◽  
Nan Li
Keyword(s):  
Azelaic Acid ◽  
Skin Irritation ◽  
Topical Administration ◽  
In Vivo Evaluation ◽  
Formulation Optimization

Topical administration of an optimal microemulsion could effectively enhance the amount of azelaic acid in skin without causing skin irritation.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

scholarly journals FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

2019 ◽  
pp. 156-163
Author(s):  
AMOL SHETE ◽  
PRIYANKA THORAT ◽  
RAJENDRA DOIJAD ◽  
SACHIN SAJANE
Keyword(s):  
Phase Separation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Separation Method ◽  
Gelling Agent ◽  
In Vivo Evaluation ◽  
Skin Delivery ◽  
Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

scholarly journals DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

scholarly journals Design and evaluation of a novel floating osmotic pump system

2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Administration ◽  
In Vitro Release ◽  
Osmotic Pump ◽  
Matrix Tablets ◽  
In Vivo Evaluation ◽  
Pump System ◽  
Conventional Tablet

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.

scholarly journals A Novel Sustained Anti-Inflammatory Effect of Atorvastatin—Calcium PLGA Nanoparticles: In Vitro Optimization and In Vivo Evaluation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1658
Author(s):  
Dalia H. Abdelkader ◽  
Ahmed Kh. Abosalha ◽  
Mohamed A. Khattab ◽  
Basmah N. Aldosari ◽  
Alanood S. Almurshedi
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
In Vitro Release ◽  
In Vivo Evaluation ◽  
Water Emulsion ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atorvastatin Calcium (At-Ca) has pleiotropic effect as anti-inflammatory drug beside its main antihyperlipidemic action. Our study was conducted to modulate the anti-inflammatory effect of At-Ca to be efficiently sustained for longer time. Single oil-water emulsion solvent evaporation technique was used to fabricate At-Ca into polymeric nanoparticles (NPs). In vitro optimization survey was performed on Poly(lactide-co-glycolide) (PLGA) loaded with At-Ca regrading to particle size, polydispersity index (PDI), zeta potential, percent entrapment efficiency (% EE), surface morphology and in vitro release pattern. In vitro drug-polymers interactions were fully scanned using Fourier-Transform Infrared Spectroscopy (FTIR) and Differential Scanning calorimetry (DSC) proving that the method of fabrication is an optimal strategy maintaining the drug structure with no interaction with polymeric matrix. The optimized formula with particle size (248.2 ± 15.13 nm), PDI (0.126 ± 0.048), zeta potential (−12.41 ± 4.80 mV), % EE (87.63 ± 3.21%), initial burst (39.78 ± 6.74%) and percent cumulative release (83.63 ± 3.71%) was orally administered in Male Sprague–Dawley rats to study the sustained anti-inflammatory effect of At-Ca PLGA NPs after carrageenan induced inflammation. In vivo results demonstrate that AT-Ca NPs has a sustained effect extending for approximately three days. Additionally, the histological examination revealed that the epidermal/dermal layers restore their typical normal cellular alignment with healthy architecture.

scholarly journals PREPARATION AND IN VIVO EVALUATION OF CANDESARTAN CILEXETIL SOLID DISPERSIONS

2021 ◽  
pp. 129-133
Author(s):  
UPPULURU ASHOK KUMAR ◽  
GANDE SURESH
Keyword(s):  
Candesartan Cilexetil ◽  
Solid Dispersions ◽  
Selective Laser Sintering ◽  
In Vitro Release ◽  
In Vivo Studies ◽  
In Vivo Evaluation ◽  
Enhanced Solubility ◽  
Pure Drug

Objective: The present study aims at development of solid dispersions (SD) of candesartan cilexetil for enhanced solubility and bioavailability. Methods: About 18 SD formulations of candesartan cilexetil were prepared by solvent evaporation technique and evaluated. The in vitro release studies were conducted and the best formulation chosen was further characterized for Fourier transform infrared spectroscopy, Scanning electron microscope, X-ray, and stability. The in vivo evaluation study conducted in rats. Results: The formulation SD16 containing drug and Soluplus in 1:3 ratio along with 2% selective laser sintering was chosen optimal based on drug content (99.08%), and drug release (99.7%). In vivo studies conducted on SD16 showed that mean time to peak concentration (Tmax) was 2.0±0.05 and 4±0.2 h for the optimized and pure drug, respectively, while mean maximum drug concentration (Cmax) was 570.63±2.65 ng/mL and was significant as compared to the candesartan pure drug 175.146±0.07 ng/mL. Area under curve AUC0-∞ infinity for candesartan SD16 was higher (4860.61±1.05 ng.h/ml) than pure drug suspension 1480±1.72 ng.h/ml. Conclusion: Hence, the developed SD formulations enhanced the bioavailability of drug by 3 folds.

A Corollary of Nanoporous Carrier Drug Delivery System: An Updated Perspective

2020 ◽  
Vol 13 (5) ◽  
pp. 5047-5061
Author(s):  
Om M Bagade ◽  
Shashikant N Dhole ◽  
Praveen D Chaudhar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Skin Irritation ◽  
Extended Period ◽  
Spherical Particles ◽  
In Vivo Evaluation ◽  
Improved Stability

Nanosponges have come into sight as one of the most promising fields of science because of their perceived applications in controlled drug delivery. It has been increasingly investigated to achieve targeted and sustained release of drugs. Nanosponges are one of the novel drug delivery system, which is gaining popularity now days because of their perceived application in controlled and site-specific drug delivery. The fundamental appeal of the nanosponge technology arises from the difficulty experienced with conventional formulations in releasing active ingredients over an extended period of time, unpleasant odor, greasiness and skin irritation. They are tiny sponge-like spherical particles with a large porous surface and are believed to contribute towards reduced side effects, improved stability, increased elegance and enhanced formulation flexibility. The present investigation in the appraisal describes nanosponge technology embracing its method of preparation, characterization, in-vitro and in-vivo evaluation methods along with recent research and future potential.

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