scholarly journals BETAMETHASONE DIPROPIONATE GEL FOR TREATMENT OF LOCALIZED PLAQUE PSORIASIS

2017 ◽  
Vol 9 (8) ◽  
pp. 173 ◽  
Author(s):  
Sanaa El Gizaway ◽  
Maha Fadel ◽  
Basma Mourad ◽  
Fatma El-zahraa Abd Elnaby
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Betamethasone Dipropionate ◽  
Average Particle ◽  
Topical Formulation ◽  
Content Type ◽  
Drug Content

Objective: The main aim of this study was to design and characterise betamethasone di-propionate loaded transfersomes (BD-T); as a topical formulation for the treatment of localized plaque psoriasis.Methods: A full factorial design (23) was applied to study the effects of three independent variables: drug content, type of surfactants and surfactant contents on particle size (PS), entrapment efficiency (EE %), zeta potential (ZP), polydispersity index (PI) and drug release profiles. The optimized BD-T was formulated as a hydrogel using 5% sodium carboxymethyl cellulose. The gel was characterized for viscosity, drug content, in vitro drug release and stability. A comparative clinical study was performed on 20 patients with psoriasis to investigate the effect of BD-T gel and the marketed betamethasone dipropionate (BD) cream.Results: The optimized BD-T formulation containing 50 mg betamethasone dipropionate (BD) and 5 mg tween 80 showed spherical unilamellar vesicles with an average particle size of 242.80, % EE of 90.19%, ZP of-15.00 mV, PI of 0.407 and K0 of 4.290 mg/hr. The formulation showed good stability at 4 °C and 25 °C for 6 mo. The results revealed significant clinical improvement and a significant increase in safety and tolerability with BD-T gel compared with BD cream.Conclusion: As a conclusion, BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.

scholarly journals Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

2021 ◽  
pp. 24-36
Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Vigna Mungo ◽  
Average Particle ◽  
Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

FORMULATION, CHARACTERIZATION AND IN VITRO EVALUTION OF GABAPENTIN FLOATING MICROSPHERES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (01) ◽  
pp. 20-27
Author(s):  
H. B Samal ◽  
I. J. Das ◽  
P. N. Murthy ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Linear Regression Method ◽  
Average Particle ◽  
Drug Entrapment Efficiency

The present study involves the design and characterization of floating microspheres with gabapentin as model drug for prolongation of gastric residence time. Gabapentin floating microspheres were prepared by o/w/o emulsification solvent diffusion technique using ethyl cellulose as the rate controlling polymer at various concentrations. The shape and surface morphology of microspheres were characterized by optical and scanning electron microscopy. Absence of drug-polymer interaction was confirmed by FTIR analysis. In vitro drug release studies were performed and drug release kinetics was evaluated using the linear regression method. Effects of polymer concentration, solvent composition, particle size, drug entrapment efficiency and drug release were also studied. The synthesized microspheres exhibited prolonged drug release (> 12 h) and remained buoyant for > 24 h. The drug entrapment efficiency was in the range 46-70 %. At higher polymer concentration, the average particle size was increased and the drug release rate decreased. In vitro studies revealed diffusion-controlled drug release from the microspheres. Among all the formulations (F1-F5), F4 is the optimized formulation.

scholarly journals Formulation and evaluation of guar gum based matrix tableted glibenclamide microspheres

2020 ◽  
Vol 11 (2) ◽  
pp. 2445-2457
Author(s):  
Prashant Singh ◽  
Ritu M. Gilgotra
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Average Particle ◽  
Drug Entrapment Efficiency

The purpose of this investigation is to establish anti-diabetic activity relationship as well as efficiency of formulated guar gum matrix tablet using microencapsulated glibenclamide (GBLD). This research is an approach to utilize pharmaceutical excipients as an alternative hypoglycemic agent. In order to execute the objective, GBLD microspheres were formulated by emulsion solvent evaporation method using dichloromethane and methanol as solvent system which was transferred drop after drop into encapsulating medium i.e. liquid paraffin light. The formulated microspheres were exposed to various assessment parameters like drug entrapment efficiency, % yield, particle size distribution, and average particle size, the morphology of surface, dissolution study (in vitro) and micromeritics of prepared microspheres. By using these microspheres, matrix tablets were then prepared which were further evaluated for weight variation, thickness, friability, hardness, drug content, stability study, disintegration time, swelling index and dissolution (in vitro) studies were carefully carried out. Betwixt all the formulated microspheres GEM3 was found to best optimized with respect to evaluation parameters. The results obtained were found within the desired ranges where % yield 93.75%, drug entrapment efficiency 95.627% at 12th hour, and the average particle size was observed to be 179.4±0.12 µm. Then, by using the method of direct compression matrix tablets of optimized microspheres GEM3 were prepared and drug release (in vitro) was performed. The obtained results of performed parameters on matrix tableted microspheres were within the acceptable range according to IP guidelines. Out of all formulated matrix tableted microspheres, formulation GMT4 and GMT7 showed an in-vitro % drug release of 95.257 and 94.404 at 12th hour in pH 7.4 phosphate buffer. 

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

scholarly journals Preparation, characterization, and in vitro evaluation of amphiphilic peptide P12 and P12-DOX nanomicelles as antitumor drug carriers

2020 ◽  
Vol 10 ◽  
pp. 184798042091151 ◽  
Author(s):  
Ping Song ◽  
Wuchen Du ◽  
Wanzhen Li ◽  
Longbao Zhu ◽  
Weiwei Zhang ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Phase ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Drug Carriers ◽  
Average Particle ◽  
Polymer Micelles ◽  
Amphiphilic Peptide

Polymerized polypeptide nanomicelles have attracted much attention as novel drug carriers because of their good biocompatibility and degradability. To prepare doxorubicin (DOX)-loaded nanomicelles, an amphiphilic peptide, FFHFFH-KKGRGD (P12), was synthesized by solid-phase synthesis, and the physicochemical and drug-release properties, as well as the cytotoxicity of the nanomicelles, were evaluated in vitro. The P12-DOX polymer micelles were prepared by dialysis. The morphology and particle size were characterized by transmission electron microscopy and dynamic light scattering. The critical micelle concentration (CMC) of the polymer was determined by the probe method, and the drug-release characteristics of the micelles were studied by dynamic dialysis. The cytotoxicity and uptake of the P12-DOX micelles were evaluated against mouse breast cancer cells (4T1) and human umbilical vein endothelial cells. The peptide polymer micelles containing DOX were uniformly sized and had a spherical core–shell structure with an average particle size of 128.6 nm. The CMC of the polymer was low (0.0357 mg/mL). The in vitro release of DOX from the micelles is slow and is consistent with first-order kinetics. The copolymer micelles of the P12 polypeptide and DOX can be used as nanoscale spherical carriers of hydrophobic drugs and have broad applicability.

Investigation on the Preparation, Characteristics, and Controlled Release Model of Paeonol-Loaded Liposome in Carbomer Hydrogel

2020 ◽  
Vol 17 (2) ◽  
pp. 159-173
Author(s):  
Qinqin Liu ◽  
Hongmei Xia ◽  
Yinxiang Xu ◽  
Yongfeng Cheng ◽  
Zhiqing Cheng
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Average Particle ◽  
Filtration Method ◽  
Ethanol Injection ◽  
Soybean Phospholipid ◽  
Release Model

Objective: Paeonol is a phenolic compounce that is volatile. In order to decrease its volatility and achieve controlled release, paeonol-loaded liposome in carbomer hydrogel was prepared by coating with soybean phospholipid via ethanol injection method and then added into the carbomer hydrogel. Methods: The quality of paeonol-loaded liposome in carbomer hydrogel was evaluated by the degree of roundness, particle size distribution, zeta potential, entrapment efficiency (filtration method and chitosan neutralization method), viscosity, infrared spectrum, etc. Furthermore, the diffusion from paeonolloaded liposome in hydrogel was studied in vitro. Results: The results showed that the average particle size of paeonol-loaded liposome was about 401 nm, the potential was -17.8 mV, and the entrapment efficiency was above 45%. The viscosity of paeonol- loaded liposome in hydrogel was 23.972×10-3 Pa*s, and the diffusion rate from paeonol-loaded liposome in hydrogel in vitro was obviously slower than that from the other paeonol preparations. Conclusion: The conclusions could be drawn that paeonol-loaded liposome in hydrogel was a kind of novel preparation, and its diffusion in vitro had obvious controlled-release characteristics, which further proved that it might improve the bioavailability of paeonol.

Design and Development of Lomustine Loaded Chitosan Nanoparticles for Efficient Brain Targeting

2020 ◽  
Vol 18 (1) ◽  
pp. 45-54 ◽  
Author(s):  
Anupriya Anand ◽  
Bharadhwaj Ramesh Iyer ◽  
Chandrasekar Ponnusamy ◽  
Rajesh Pandiyan ◽  
Abimanyu Sugumaran
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
P Value ◽  
Drug Content ◽  
Diffusion Controlled

Aim: The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design. Methods: The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release. Results: The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1. Conclusion: In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.

scholarly journals Formulation and Evaluation of Nanosuspension as an Alternative Approach for Solubility Enhancement of Simvastatin

2021 ◽  
Vol 71 (1) ◽  
Author(s):  
Mohini E. Shinde ◽  
Mitesh P. Sonawane ◽  
Avish D. Maru
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Average Particle ◽  
Particle Size Reduction ◽  
Drug Effectiveness ◽  
Saturation Solubility ◽  
Drug Content ◽  
Poorly Water Soluble

Solubility is an essential factor for drug effectiveness. Simvastatin is poorly water-soluble drug and its bioavailability is very low. Nanosuspension is one of those approach which can tremendously enhance the effective surface area of drug particles by reducing the particle size and there by increases the rate of dissolution and hence improve bioavailability. The main purpose of the present investigation was to increase the saturation solubility of simvastatin by preparation of nanosuspension. Nanosuspension of simvastatin were prepared by nanoprecipitation method using hydroxypropyl cellulose as stabilizer and sodium lauryl sulphate as surfactant. Prepared nanosuspension was evaluated for its particle size, total drug content, entrapment efficiency and saturation solubility study. On the basis of the evaluation, the best batch F8 formulation demonstrated highest drug content and entrapment efficiency with average particle size of 0.004µm. The saturation solubility studies show the solubility of the prepared nanosuspension has increased as compared to the pure drug due to the particle size reduction. The nanosuspension of simvastatin could be successfully prepared and can be concluded that the nanosuspension formulation is a promising approach to enhance the solubility. The nanoprecipitation is a simple and effective method to produce nano sized particles of poorly water-soluble drugs with enhance solubility.

scholarly journals A NOVEL NANOGEL FORMULATION OF FINASTERIDE FOR TOPICAL TREATMENT OF ANDROGENETIC ALOPECIA: DESIGN, CHARACTERIZATION AND IN VITRO EVALUATION

2021 ◽  
pp. 228-240
Author(s):  
DIVYA SANGANABHATLA ◽  
R. SHYAM SUNDER
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Androgenetic Alopecia ◽  
Stability Studies ◽  
Drug Content ◽  
Release Study

Objective: The present paper describes the development and evaluation of a Novel Finasteride (FSD) nanogel topical delivery for the treatment of Androgenetic Alopecia. Nano-based topical formulation was chosen to enhance the solubility, permeability, biocompatibility of drug and to overcome the problems associated with the oral delivery of finasteride. Methods: Various trails batches were prepared by using probe sonication method. Based on stability studies and particle size, NP4 trail was optimized which exhibited a spherical shape with a mean diameter of 113.80±0.72, the polydispersity of 0.28±0.01, zeta potential of-25.2 mV, drug entrapment efficiency of 92.67±0.47 %, and drug loading of 6.15±0.02 %. Storage stability studies demonstrated that the particle size and entrapment efficiency were not changed during 3 mo both at 4 °C and room temperature. Finasteride (FSD) NLCs were characterized for particle size by scanning electron microscope (SEM), chemical state by X-Ray diffraction (XRD), physical stability by centrifugation and thermodynamic stability by Freeze-thaw method. These prepared nanoparticles were transformed into topical nanogel and further evaluated. Results: Among the different trails, C2 trail of NLC gel has shown excellent gelling capacity, clear appearance, good viscosity characteristics and was selected for further evaluation studies. Batches of topical nanogel were characterized through pH, homogeneity, spreadability, viscosity, drug content and in vitro drug release study. Based on pH (6.5-6.8), drug content (91.25±0.9%), spreadability (6.7 cm/sec), C2 batch was subjected to In vitro skin occlusivity study, in-vitro release study and In vitro heamolysis study. Conclusion: The percent cumulative drug release for Finasteride (FSD) gel was found to be 758.52±1.49 µg at 24 h which is quite higher than plain gel and Finasteride (FSD) gel showed maximum occlusiveness and excellent spreadability and found to be stable. In conclusion, prepared Finasteride (FSD) Nanogel could be used with promising potential for the treatment of Androgenetic Alopecia.

Formulation and Evaluation of Ketoprofen Using β-Cyclodextrin Capped Silver Nanoparticles

2021 ◽  
Vol 14 (3) ◽  
pp. 5501-5507
Author(s):  
Kiranmai Mandava ◽  
Kruthika Lalit ◽  
Venu Madhav Katla
Keyword(s):  
Particle Size ◽  
Silver Nanoparticles ◽  
Average Particle Size ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Average Particle ◽  
Dissolution Studies ◽  
Drug Entrapment Efficiency

The objective of the study was to develop silver nanoparticles loaded with Ketoprofen (Ag-KP) for increasing the drug solubility and thereby its bioavailability. Ag-KP were prepared by the solvent evaporation method using β-Cyclodextrin as a biodegradable polymer. Different formulations of Ag-KP were characterized for the drug entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), particle size analysis, X-ray diffraction studies (XRD), scanning electron microscopy (SEM) and  in-vitro dissolution studies. The optimized formulation (F6) has shown an average particle size of 167.8 ± 3.46 nm,zeta potential of -23.7 ± 1.46 mV. FTIR revealed that the drug showed good excipient compatibility. XRD studies showed that the drug has changed from crystalline to amorphous state. In all formulations, F6 formulation (optimized) exhibited high drug entrapment efficiency (∼93%). SEM studies indicated the shape of Ag-KP was roughly spherical with smooth surface. In vitro dissolution studies showed that Ag-KP from F6 formulation was 94.3 ± 4.9% but for the marketed formulation, it is only 84.6 ± 3.7% in 12 hours and F6 was found to be found stable for three months at both refrigerated and room temperature (RT).

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