scholarly journals FORMULATION, OPTIMIZATION, CHARACTERIZATION AND IN VIVO ANTI-ULCER ACTIVITY OF ESOMEPRAZOLE MAGNESIUM TRIHYDRATE GASTRORESISTANT MICROSPHERES

2016 ◽  
Vol 9 (1) ◽  
pp. 273
Author(s):  
Krutika Sawant ◽  
Mitali Patel ◽  
Jiten Patel ◽  
Piyush Mundada
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Intestinal Absorption ◽  
Ulcer Formation ◽  
Scanning Calorimetry ◽  
Aqueous Solvent ◽  
Release Study ◽  
Esomeprazole Magnesium

<p><strong>Objective: </strong>The objective of the present investigation was to prepare gastro-resistant microspheres of esomeprazole magnesium trihydrate (EMT) to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption.</p><p><strong>Methods: </strong>EMT loaded gastro-resistant microspheres were prepared using hypromellose acetate succinate (HPMCAS) as the gastro-resistant polymer by ‘non-aqueous solvent evaporation’ technique. A 3-factor 3 level factorial design was used to optimise EMT: HPMCAS ratio, the concentration of Span 80 and stirring speed with respect to percent entrapment efficiency and particle size. Further characterization was carried out using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), <em>In vitro</em> release study and <em>In vivo</em> anti-ulcer activity.</p><p><strong>Results: </strong>Fourier transform infrared <strong>(</strong>FTIR) study indicated compatibility between drug and polymer. DSC study revealed that the drug was molecularly dispersed in the polymer. The optimised batch showed 49.63±1.23% drug entrapment and 170.12±3.36 μm particle size. SEM study showed that microspheres were spherical in shape<strong>. </strong><em>In vitro</em> drug release study showed only 4.28±1.23% drug release in simulated gastric media in 2 hr and 93.46±1.20% release in simulated intestinal media after 1 hr from the optimised batch.</p><p><strong>Conclusion: </strong>Results of <em>in vitro </em>release studies indicated the gastro-resistant nature of the developed microspheres. <em>In vivo</em> anti-ulcer activity demonstrated that EMT loaded microspheres were able to significantly reduce ethanol-induced ulcer formation in rats’ stomach as compared to the aqueous solution of EMT. So it can be concluded that the developed gastro-resistant microspheres of EMT prevented drug release in the stomach which would lead to a significant improvement in its bioavailability through enhanced intestinal absorption</p>

scholarly journals DEVELOPMENT OF RITONAVIR LOADED NANOPARTICLES: IN VITRO AND IN VIVO CHARACTERIZATION

2018 ◽  
Vol 11 (3) ◽  
pp. 284
Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Dissolution Rate ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Significant Rise ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.

scholarly journals DEVELOPMENT OF MESALAZINE MICROSPHERES FOR COLON TARGETING

2017 ◽  
Vol 9 (4) ◽  
pp. 1
Author(s):  
Katta Rajesh ◽  
R. Deveswaran ◽  
S. Bharath ◽  
B. V. Basavaraj
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Delivery ◽  
Scanning Calorimetry ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Aqueous Solvent ◽  
S 100 ◽  
Span 80 ◽  
Eudragit S 100

Objective: The present work was aimed at preparation of mesalazine microspheres by a non-aqueous solvent evaporation method using eudragit S 100 and eudragit L 100 as pH dependent polymers for colon targeting.Methods: The ratio of drug to polymer was varied and the effect of formulation variables revolutions per minute (RPM) (1000, 1500, 2000 and 2500) and concentration of span 80 (1%, 1.5%, 2% and 2.5%) were studied. Prepared microspheres were evaluated for particle size, percent drug entrapment, granular analysis, in vitro drug release studies, Fourier transformed infrared spectroscopy (FT-IR) Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) studies.Results: Particle size has decreased and percent drug entrapment had increased with increase in RPM in all formulations. When the span 80 concentration increased, the particle size of the microsphere formulations increased and percent drug entrapment decreased in eudragit S 100 microspheres; whereas in eudragit L 100 microspheres, as the concentration of span 80 increased, the particle size of the microsphere formulations decreased. The prepared microspheres sustained the drug release over a period of 12 h.Conclusion: Thus eudragit S 100 and eudragit L 100 microspheres could constitute a promising approach for colon-specific and sustained delivery of mesalazine for the treatment of inflammatory bowel disease.

scholarly journals Development, Optimisation and Evaluation of Ketoprofen Lipospheres

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1853-1863
Author(s):  
Shubhra Rai ◽  
Gopal Rai ◽  
Ashish Budhrani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Research Work ◽  
Extended Period ◽  
Entrapment Efficiency ◽  
Inflammatory Activity ◽  
Scanning Calorimetry ◽  
Anti Inflammatory

Lipospheres represent a novel type of fat-based encapsulation system produced for the topical drug delivery of bioactive compounds. The goal of this research work was to develop lipospheres, including ketoprofen applied for topical skin drug delivery. Ketoprofen lipospheres were formulated by melt emulsification method using stearic acid and Phospholipon® 90G. The lipospheres were analysed in terms of particle size and morphology, entrapment efficiency, Differential scanning calorimetry, In-vitro drug release, In-vivo (Anti-inflammatory activity). Outcomes of research revealed that particle size was found to be 9.66 µm and entrapment efficiency 86.21 ± 5.79 %. In-vivo, the study of ketoprofen loaded lipospheres formulation shows a higher plain formulation concentration in plasma (5.61 mg/mL). For dermis, ketoprofen retention was 27.02 ± 5.4 mg/mL for the lipospheres formulation, in contrast to that of the plain formulation group (10.05 ± 2.8 mg/mL). The anti-inflammatory effect of liposphere drug delivery systems was assessed by the xylene induced ear oedema technique and compared with marketed products. Finally, it seems that the liposphere drug delivery system possesses superior anti-inflammatory activity as compared to the marketed product gel consistencies. Liposphere may be capable of entrapping the medicament at very high levels and controlling its release over an extended period. Liposphere furnishes a proper size for topical delivery as well as is based on non-irritating and non-toxic lipids; it’s a better option for application on damaged or inflamed skin.

scholarly journals Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Santanu Chakraborty ◽  
Priyanka Nayak ◽  
Bala Murali Krishna ◽  
Madhusmruti Khandai ◽  
Ashoke Kumar Ghosh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Polymer Concentration ◽  
Research Work ◽  
In Vivo Studies ◽  
Systemic Absorption ◽  
Cross Linking ◽  
Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. <em>In vitro</em> drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t<sub>50%</sub> values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

scholarly journals Enhanced Oral Bioavailability of Celecoxib Nanocrystalline Solid Dispersion based on Wet Media Milling Technique: Formulation, Optimization and In Vitro/In Vivo Evaluation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 328 ◽  
Author(s):  
Zhuang Ding ◽  
Lili Wang ◽  
Yangyang Xing ◽  
Yanna Zhao ◽  
Zhengping Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Stability Study ◽  
Sprague Dawley ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.

scholarly journals FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

2019 ◽  
Vol 9 (4-A) ◽  
pp. 425-437
Author(s):  
Khushboo Verma ◽  
Jhakeshwar Prasad ◽  
Suman Saha ◽  
Surabhi Sahu
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Mean Particle Size ◽  
Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

scholarly journals FORMULATION AND OPTIMIZATION OF NANOSUSPENSION FOR IMPROVING SOLUBILITY AND DISSOLUTION OF GEMFIBROZIL

2019 ◽  
Vol 12 (1) ◽  
pp. 157 ◽  
Author(s):  
Sanjeevani S Deshkar ◽  
Kiran G Sonkamble ◽  
Jayashri G Mahore
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Chemical Change ◽  
Fold Increase ◽  
Sonication Time ◽  
Scanning Calorimetry ◽  
Solubility In Water ◽  
Pure Drug

Objective: The study aims at the formulation and optimization of gemfibrozil (Gem) nanosuspension (NS) for improving its solubility and dissolution rate.Method: Gem NS was prepared by precipitation-ultrasonication method using ethanol as solvent, water as anti-solvent, and polyvinyl alcohol (PVA) as a stabilizer. A Box–Behnken design was employed to study the effect of the independent variables, Gem concentration in the organic phase (X1), PVA concentration (X2) and sonication time (X3) on the dependent variable, drug release after 90 min (Y). The resulting data were statistically analyzed and subjected to 3D response surface methodology to study the influence of variables on the response. NS was evaluated for particle size, zeta potential, solubility and in vitro drug release and characterized using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffractometry (XRD).Results: On the basis of the evaluation, NS4 formulation (with 80 mg/ml Gem, 0.5% PVA concentration, and 20 min of sonication time) demonstrated highest drug content with a particle size of 191.0 nm and zeta potential of −12.0 mV. Dissolution profiles of NS indicated 2.5-fold increase in drug release than pure drug. NS demonstrated 5- and 9-fold increase in solubility, in water, and phosphate buffer (pH 7.5), respectively, pure drug. DSC and XRD studies indicated changes in the crystallinity of Gem during NS formulation. No chemical change was evident in NS as indicated by FTIR.Conclusion: Gem NS formulation could serve as a promising approach for improving its solubility and dissolution rate.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

An Innovative Approach for Development and Evaluation of Nanosized Lamotrigine Loaded Bionanoparticles Using Biopolymer from Fragaria × ananassa Fruit

2020 ◽  
Vol 13 (4) ◽  
pp. 4990-4999
Author(s):  
Sushant Kumar ◽  
Satheesh Madhav N V ◽  
Anurag Verma ◽  
Kamla Pathak
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Kinetic Study ◽  
In Vitro Release ◽  
Release Kinetic ◽  
Fruit Pulp ◽  
Fragaria Ananassa ◽  
Release Study ◽  
Vitro Release

The purpose of this research was to isolate the smart biopolymer from the fruit pulp of Fragaria × ananassa (garden strawberry). We isolated natural fruit pulp to evaluate the potentiality of biopolymer in delivery of nanosized lamotrigine as an antiepileptic drug. Lamotrigine was nanosized by screening its nano-size particle by UV method. The nanosized lamotrigine was used for preparation of bionanoparticles (LF1-LF8) by sonication method. The isolated biopolymer was characterized for DSC, FTIR, NMR, Mass and Zeta particle size analysis. The obtained results confirm its polymeric nature in different analysis. The prepared bionanoparticles showed the release of lamotrigine in sustained manner over 36 hours. The release kinetic study was done by using the BIT-SOFT 1.12 software and T50% and T80%, r2 were calculated. All the formulation showed more than 99.78% drug release. The In-vitro release study of different formulations showed the % drug release from 90.92% to 99.78%. The different formulations were evaluated for the In-vitro release study and release kinetic was studied. The formulation LF5 was found to be the best formulation having T50% of 17 hours and T80% of 29 hours with r2 value of 0.9925. The best formulation LF5 showed up to 90.925% drug release over 36 hours. According to the release kinetic study, the best-fit model was found to be Koresmayer-Peppas and the mechanism of drug release was found to be anomalous transport. The results obtained from different evaluations like percentage entrapment efficiency, particle size, release study, kinetic studies and stability study revealed that isolated biopolymer has good potentiality to form bionanoparticles and it can be safely used as an alternative to synthetic and semisynthetic polymers for the preparation of lamotrigine loaded stable bionanoparticles

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