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

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.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v12i1.26724 ◽

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

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FORMULATION AND CHARACTERIZATION OF PAPAIN LOADED SOLID LIPID NANOPARTICLES AGAINST HUMAN COLORECTAL ADENOCARCINOMA CELL LINE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i10.27258 ◽

2018 ◽

Vol 11 (10) ◽

pp. 393

Author(s):

Suriyakala Perumal Chandran ◽

Kannikaparameswari Nachimuthu

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Cell Viability ◽

Cell Line ◽

Solid Lipid Nanoparticles ◽

Colorectal Adenocarcinoma ◽

Lipid Nanoparticles ◽

In Vitro Drug Release

Objective: Colorectal cancer is one of the most commonly diagnosed cancer and also most common gastrointestinal malignancy with high prevalence rate in the younger population. Usually, cancer cells are surrounded by a fibrin coat which is resistant to fibrinolytic degradation. This fibrin coat is act as self-protective against natural killing mechanism. The main objective was to prepare papain-loaded solid lipid nanoparticles (P-SLN) by melt dispersion-ultrasonication method and investigated the cytotoxic efficacy against colorectal adenocarcinoma (human colorectal adenocarcinoma [HCT 15]) cells.Methods: Optimized polymer ratio was characterized by differential scanning calorimetry, Fourier-transform infrared, X-ray diffraction, scanning electron microscopy, entrapment efficiency, particle size and zeta potential analysis, in vitro drug release, and in vitro cytotoxicity studies on HCT-15 colorectal adenocarcinoma cells.Results: The results showed that the particle size, morphological character and zeta potential value of optimized batch P-SLN were 265 nm, spherical and −26.5 Mv, respectively. The in vitro drug profile of P-SLN exhibited that it produced sustain drug release, and the cell viability of HCT-15 against P-SLN shown better efficacy than pure papain enzyme.Conclusion: P-SLNs were successfully prepared and investigated the in vitro drug release and in vitro cell viability against HCT-15 cell line.

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pH-Responsive Liposomes of Dioleoyl Phosphatidylethanolamine and Cholesteryl Hemisuccinate for the Enhanced Anticancer Efficacy of Cisplatin

Pharmaceutics ◽

10.3390/pharmaceutics14010129 ◽

2022 ◽

Vol 14 (1) ◽

pp. 129

Author(s):

Hassan Shah ◽

Asadullah Madni ◽

Muhammad Muzamil Khan ◽

Fiaz-ud-Din Ahmad ◽

Nasrullah Jan ◽

...

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Release Rate ◽

In Vitro Release ◽

Chemotherapeutic Agents ◽

Ph Responsive ◽

Scanning Calorimetry ◽

Cholesteryl Hemisuccinate ◽

Vitro Release

The current study aimed to develop pH-responsive cisplatin-loaded liposomes (CDDP@PLs) via the thin film hydration method. Formulations with varied ratios of dioleoyl phosphatidylethanolamine (DOPE) to cholesteryl hemisuccinate (CHEMS) were investigated to obtain the optimal particle size, zeta potential, entrapment efficiency, in vitro release profile, and stability. The particle size of the CDDP@PLs was in the range of 153.2 ± 3.08–206.4 ± 2.26 nm, zeta potential was −17.8 ± 1.26 to −24.6 ± 1.72, and PDI displayed an acceptable size distribution. Transmission electron microscopy revealed a spherical shape with ~200 nm size. Fourier transform infrared spectroscopic analysis showed the physicochemical stability of CDDP@PLs, and differential scanning calorimetry analysis showed the loss of the crystalline nature of cisplatin in liposomes. In vitro release study of CDDP@PLs at pH 7.4 depicted the lower release rate of cisplatin (less than 40%), and at a pH of 6.5, an almost 65% release rate was achieved compared to the release rate at pH 5.5 (more than 80%) showing the tumor-specific drug release. The cytotoxicity study showed the improved cytotoxicity of CDDP@PLs compared to cisplatin solution in MDA-MB-231 and SK-OV-3 cell lines, and fluorescence microscopy also showed enhanced cellular internalization. The acute toxicity study showed the safety and biocompatibility of the developed carrier system for the potential delivery of chemotherapeutic agents. These studies suggest that CDDP@PLs could be utilized as an efficient delivery system for the enhancement of therapeutic efficacy and to minimize the side effects of chemotherapy by releasing cisplatin at the tumor site.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i3.23145 ◽

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.

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PREPARATION, PHYSICAL CHARACTERIZATION, AND PHARMACOKINETIC STUDY OF DOCETAXEL NANOCRYSTALS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i6.32856 ◽

2019 ◽

pp. 238-244

Author(s):

ARVIND GANNIMITTA ◽

PRATHIMA SRINIVAS ◽

VENKATESHWAR REDDY A ◽

PEDIREDDI SOBHITA RANI

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Water Solubility ◽

Release Kinetics ◽

Tween 80 ◽

Fickian Diffusion ◽

Sustained Drug Release ◽

Egg Lecithin

Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel. Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release. Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian). Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11s4.31721 ◽

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..

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

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i1.15437 ◽

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

Objective: 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.Methods: 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), In vitro release study and In vivo anti-ulcer activity.Results: Fourier transform infrared (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. In vitro 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.Conclusion: Results of in vitro release studies indicated the gastro-resistant nature of the developed microspheres. In vivo 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

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FABRICATION AND IN VITRO CHARACTERIZATION OF A NOVEL NANOSUSPENSION OF TELMISARTAN: A POORLY SOLUBLE DRUG PREPARED BY ANTISOLVENT PRECIPITATION TECHNIQUE USING 33 FACTORIAL DESIGN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i5.38865 ◽

2020 ◽

pp. 286-294

Author(s):

PRASANTA KUMAR MOHAPATRA ◽

SIREESHA ◽

VAIBHAV RATHORE ◽

HARISH CHANDRA VERMA ◽

BIBHUTI PRASAD RATH ◽

...

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Dissolution Rate ◽

Release Kinetics ◽

Precipitation Method ◽

Lauryl Sulfate ◽

Poorly Soluble ◽

Poorly Soluble Drug

Objective: The motivation behind the current examination was to build the solvency and dissolution rate of an antihypertensive drug telmisartan by the planning of nanosuspension by precipitation method at the research facility scale. We researched the nanoparticle manufacture of telmisartan employing a 33 factorial experimental configuration considering the impacts of nanosuspension on the physical, morphological, and dissolution properties of telmisartan. Methods: To get ready, nanosuspension particles of an ineffectively dissolvable drug are moreover of a drug solution to the anti-solvent leads to abrupt supersaturation and precipitation the making of nanoparticles. The nanosuspension particles of a poorly soluble drug loaded with urea and surfactants (sodium lauryl sulfate (SLS), poloxamer 188, Tween 80) have been prepared by a precipitation method. The nanosuspension particles were characterized for particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), in vitro drug release, and release kinetics. Results: The readily optimized batch nanosuspension particles evaluated and exhibited the particle size (750 nm), zeta potential (-24.33 mV), differential scanning calorimetry (DSC) drug exhibited a change in crystalline form to amorphous, in vitro dissolution (F12 was higher 95% within 5 min) and drug release kinetics. The formulation parameter of surfactant concentration is optimized. Conclusion: The formulation of the nanosuspension approach has been shown to substantial improvement in the dissolution rate, thereby enhancing the oral bioavailability with the future development of this technology.

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

Pharmaceutics ◽

10.3390/pharmaceutics11070328 ◽

2019 ◽

Vol 11 (7) ◽

pp. 328 ◽

Cited By ~ 9

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.

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Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

Advances in Pharmaceutics ◽

10.1155/2015/363061 ◽

2015 ◽

Vol 2015 ◽

pp. 1-7 ◽

Cited By ~ 2

Author(s):

Gajanan Shinde ◽

Mitesh Patel ◽

Manan Mehta ◽

Rajesh Kesarla ◽

Ganesh Bangale

Keyword(s):

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

Polymer Concentration ◽

Study Data ◽

Stability Study ◽

Diabetes Therapy ◽

Peg 4000 ◽

Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

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