scholarly journals PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES

2017 ◽  
Vol 10 (3) ◽  
pp. 103 ◽  
Author(s):  
Megha Sharma ◽  
Seema Kohli ◽  
Abhisek Pal
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Gastric Fluid ◽  
Appreciable Amount ◽  
Average Particle

ABSTRACTObjective: To develop and evaluate floating microspheres of repaglinide (RG).Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMCK4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirringspeed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infraredspectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. Theresults showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from themicrospheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailabilityand patient compliance.Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.

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.

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.

scholarly journals Improvement in Entrapment Efficiency and In Vitro Digestion Stability of Lutein by Zein Nanocarriers with Pepsin Hydrolysis

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Yan Jiao ◽  
He Han ◽  
Ying Chang ◽  
Dajing Li ◽  
Asad Riaz
Keyword(s):  
Structural Characteristics ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
In Vitro Digestion ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Average Particle ◽  
Simulated Intestinal Fluid ◽  
Bioactive Ingredients

Zein is one of the popular bioactive carriers and play critical roles in the promotion of stability, absorption, and utilization of the nutrients and bioactive ingredients. The application of zein delivery systems for the encapsulation of bioactive ingredients has recently gained increasing interest. The aim of this work was to modify zein by pepsin and prepare the lutein-loaded zein nanoparticle (LZN) and the lutein-loaded zein hydrolysate nanoparticle (LZHN), respectively. The effects of zein hydrolysation on entrapment efficiency and in vitro digestion stability of lutein were also evaluated in this study. Hydrolysation of zein by the pepsin has important effects on lutein embedding. The optimal hydrolysis conditions, including the pepsin concentration (1.5%), temperature (55°C), and time (4 h), enhanced the entrapment efficiency (EE) of lutein by 93.82 ± 2.82% as compared to 85.18 ± 3.28% of the untreated zein, respectively. In contrast to LZN, LZHN had better structural characteristics, the average particle size decreases from 158.40 ± 3.22 nm to 112.2 ± 1.56 nm, and LZHN showed better dispersivity and zeta potential. The stability and release assays in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) showed that hydrolyzed zein nanocarriers by pepsin improved the digestion stability and promoted the release of lutein under gastrointestinal digestive conditions. These results suggest that hydrolyzed zein with pepsin may act as an effective carrier for lutein delivery and shows many potential advantages compared with the zein.

scholarly journals Formulation and Evaluation of Ketoconazole Nanosponge gel

2021 ◽  
Vol 23 (2) ◽  
Author(s):  
Vijay R Chakote ◽  
◽  
Ms.Deepali R. Wagh ◽  
Mr. Rahul S. Waghmare ◽  
Umesh T. Jadhao ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Average Particle ◽  
Sustained Drug Release ◽  
Percentage Yield ◽  
Viscosity Study ◽  
Cross Linker

Ketoconazole Nanosponges were prepared by using Hyper cross linked β-cyclodextrin method by using different concentration of cross-linker. Diphenyl carbonate was used as the cross linking polymer. Nanosponge formulations were prepared by using β-CD: cross linker ratios of 1:15, 1:10, 1:5 and 1:3.Thepreparednanosponges were evaluated for percentage yield, incorporation efficiency, particle size, drug polymer compatibility, scanning electron microscopy andin-vitrodrugrelease.SEM studies confirmed their porous structure with number of nano channels. The FTIR spectra showed stable character of Ketoconazole in mixture of polymers and revealed the absence of drug polymer interactions. DSC study revealed that drug was involved in complexation with nanosponges. The average particle size of Ketoconazole nanoparticles was found to be in the range of 78.81± 0.20 nm to336.02 ± 0.124nm.The drug release from nanosponges was found to extended upto 8hr. 82 to 92%.The nano sponges were formulated into gel using Carbopol 940Batches G1 to G4 were prepared by incorporating nanosponges equivalent to 6%w/w of ketoconazole in different polymer concentrations respectively and evaluated for Percent drug content, Viscosity study, Spreadability study, In vitro diffusion studies. Nanosponge gel G1 showed the optimum pH, viscosity, Spread ability and In vitro release. Drug diffusion from the nanosponge loaded gel formulations was show sustained rate. A sustained release topical drug delivery of Ketoconazole developed as a nanosponge loaded gel offers solubilizing matrix for the drug, served as a local depot for sustained drug release and provided a rate limiting matrix barrier for modulation of drug release.

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 Formulation and Evaluation of Mucoadhesive Acarbose Microspheres

2016 ◽  
Vol 1 (1) ◽  
Author(s):  
Manish Kumar Sharma
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Average Particle Size ◽  
Prolonged Release ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
In Vitro Adhesion

The purpose of the present investigation was the formulation and characterization of mucoadhesive sustained release microsphere of antidibetic drug Acarbose that would adhere in mucosa and release continuously to provide long term effect. There was various formulations of Acarbose were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC), Sodium Alginate, Carbopol, Xanthan gum, Guar gum as a polymer. The prepared mucoadhesive microspheres were evaluated for particle size, surface morphology, drug entrapment efficiency, Drug content, buoyancy percentage and In-vitro drug release, In-vitro adhesion test and stability studies. The particle was found to be discrete and spherical with the average particle size in the range of 105.5 to 413.5μm. As the concentration of polymers increases it affects the various evaluation parameters like particle size, in-vitro drug release and In-vitro adhesion. The floating microspheres of optimized formulation exhibited the prolonged release of 85.8% in continuous manner up to 12 hrs. It is concluded that the optimized formulation of Acarbose mucoadhesive microspheres can be selected for sustained drug delivery system for improved bioavailability.

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 OPTIMIZATION AND IN VITRO CHARACTERIZATION OF OLANZAPINE LIPOSOME

2021 ◽  
pp. 109-114
Author(s):  
G. NETHRA VANI ◽  
M. ALAGUSUNDARAM ◽  
K. B. CHANDRASEKAR
Keyword(s):  
Zeta Potential ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Prediction Method ◽  
Entrapment Efficiency ◽  
Zero Order ◽  
Nasal Delivery ◽  
Brain Targeting ◽  
Average Particle

Objective: Olanzapine (OZ) is a thioeno benzodiazepine class second-generation or atypical antipsychotic that selectively binds to central dopamine D2 and serotonin (5-HT2c) receptors used for the treatment of schizophrenia and bipolar disorder. The present paper is aimed at developing an optimized liposome-loaded OZ as an approach for brain targeting through the nasal route for effective therapeutic management of schizophrenia. Methods: The OZ liposomes were prepared by the thin-film hydration method. Various independent variable such as phospholipid, cholesterol and sonication time was optimized by using Design-Expert® Software to obtain the dependent variables of entrapment efficiency, vesicle size and zeta potential. The optimized formulation was predicted based on the response obtained by the point prediction method. Results: The entrapment efficiency of the formulation was range between 72.9 and 85.1 %. The average particle size of all the 15 experimental runs lies between the minimum and maximum values of the size 258.33 to 325.32 nm, respectively. The zeta potential ranges from-27.53 to-11.46 mV. The optimized formulation for characterized for its morphology by Transmission Electron Microscopy (TEM). In vitro release studies of OZ-loaded liposomal formulation was carried by dialysis sac method using pH 7.4 phosphate buffer (PBS) as a medium. The maximum release was found to be 98.43±1.2 % up to 24 h. The R2 zero-order kinetics and Korsmeyer-Peppas model was found to be 0.9919 and 0.9664, respectively. The zero-order shows the best-fit model with a highest R2 value exhibiting better correlation and the ‘n’ value was also found to be 0.85; indicating both diffusion-controlled and swelling-controlled drug release that is anomalous transport. Conclusion: The results, clearly states that the prepared formulations justify the parameters and OZ might be a suitable candidate to target the brain through nasal delivery.

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. 

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

Drug Research ◽  
2020 ◽  
Author(s):  
Sonia Pahuja ◽  
Shweta Aggarwal ◽  
Prerna Sarup
Keyword(s):  
Average Particle Size ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Average Particle ◽  
Chitosan Microspheres ◽  
Optimum Parameters ◽  
Sustained Effect

Abstract Objective The present investigation entailed determination of effect of diverse cross-linking agents on Losartan Potassium loaded chitosan microspheres. The emulsion cross-linking method was employed to formulate the microspheres with an endeavour to achieve maximum sustained effect. Methods The FTIR studies revealed absence of any interaction between Losartan and chitosan. The emulsion cross linking method was accomplished in three steps encompassing formation of an aqueous and oily phase, emulsification and cross-linking. A total of eighteen Losartan formulations were developed using six different cross-linkers at three varying level were screened for optimum parameters. The in vitro drug release parameters of optimum formulations (LC3, LE3, LF3, LG3, LS3 and LV3) containing citric acid, epichlorohydrin, formaldehyde, glutaraldehyde, suphuric acid and vanillin as cross-linkers were assessed to determine the sustained effect. Results The values of evaluated parameters including percent yield (94.67%), average particle size (51.19 µm), drug content (44.38 mg) and entrapment efficiency (88.77%) connoted LG3 as the best formulation. Additionally, the values of relative measure of skewness (β1=0.01 and γ1=0.10) and platykurtic (β2=1.26) size distribution were least for LG3 with spherical shape and smooth surface as revealed by SEM studies. Conclusion The outcome of in vitro release and other characterizations of microspheres explicitly revealed glutaraldehyde as the best cross-linker amongst the cross-linkers used herewith. The maximum sustained effect (lasting over a period of 24 h) accompanied with higher MDT and t50% with lower%DE and Q14h values thus corroborated the objective of attaining sustained release of Losartan.

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