scholarly journals Galactosylated Albumin Nanoparticles Bearing Cimetidine

2014 ◽  
Vol 2 (5) ◽  
pp. 202-229
Author(s):  
Kumar Ganesh ◽  
Dhyani Archana ◽  
Kathiyal Preeti
Keyword(s):  
Drug Loading ◽  
Polymer Concentration ◽  
Life Sciences ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Albumin Nanoparticles ◽  
Coated Nanoparticles ◽  
Percentage Yield ◽  
Selective Delivery

The galacotsylated albumin nanoparticles were prepared for the selective delivery of Cimetidine to the asialoglycoprotein receptor (ASGP-R) which is particularly presents on mammalian hepatocytes. The albumin nanoparticles (NPs) were prepared by using desolvation method and efficiently conjugated with galactose. Various parameters such as particle size, % entrapment efficiency and drug loading efficiency, percentage yield, in vitro drug release, were determined. The size of nanoparticles (both plain and galactose coated) was found to be in range of 200-250 nm, and maximum drug payload was found to be 19.08% ± 1.10 .The maximum drug content was found to be 30.80% ± 0.3 and 27.09% ± 0.5 respectively in plain and galactose coated nanoparticles while the maximum entrapment efficiency was found to be 90.68% ± 0.5 and 91.75% ± 0.59 in plain and coated nanoparticles. It was also found that coating of nanoparticles increases the size of nanoparticles. From the in-vitro studies, it was concluded that increase in polymer concentration, decreases the drug releases from the nanoparticles. DOI: http://dx.doi.org/10.3329/ijpls.v2i5.17628 International Journal of Pharmaceutical and Life Sciences, Volume 2(5) Dec 2013: 202-229

scholarly journals Formulation and Evaluation of Ranitidine Hydrochloride Loaded Floating Microspheres for the Treatment of Gastric Ulcer

2021 ◽  
Vol 04 (08) ◽  
Author(s):  
Manikandan Palanivelu ◽  
Keyword(s):  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Ranitidine Hydrochloride ◽  
Percentage Yield ◽  
Evaporation Technique ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

The study was aimed to prepare gastro retentive floating microsphere of Ranitidine Hydrochloride by Ionotropic Gelation technique and solvent evaporation technique by using the different carriers’ ratios (Carbopol 934, Chitosan, and sodium alginate). Both natural and synthetic polymers have been used to prepare floating microspheres and evaluated the relevant parameters. There was no drug and carrier interactions assessed from FTIR. Depending upon the ratio, the percentage yield was found between 58.33% to 90.38%. in all formulations. The surface morphology of microspheres was characterized by SEM and it was discrete, spherical in shape with rough outer surface and showed free flowing properties. The mean particle size of microspheres significantly increases with increasing polymer concentration and the range between 99.92±1.221 to 168.23±1.963 µm. Among all the formulations, RF3 showed high drug entrapment efficiency (87.52%). The percentage in-vitro buoyancy of the floating microspheres was in the range of 66.92% to 81.52%. The in-vitro drug release study revealed that RF3, RF6 and RF9 Formulations having 89.97%,92.91%,93.68% drug released at the end of dissolution studies respectively. It could be concluded that the developed floating microsphere of Ranitidine Hydrochloride can be used for prolonged release in stomach. Therefore improving the bioavailability and patient compliance.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

PREPARATION AND IN VITRO EVALUATION OF BIODEGRADABLE ZIDOVUDINE LOADED CONTROLLED RELEASE MICROSPHERES USING NATURAL GUMS AS RELEASE RETARDANTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (06) ◽  
pp. 37-45
Author(s):  
S. M. Sai ◽  
◽  
R. P Swain ◽  
A. K Mahapatra
Keyword(s):  
Sodium Alginate ◽  
Guar Gum ◽  
Particle Diameter ◽  
Kinetic Studies ◽  
Entrapment Efficiency ◽  
Processing Parameters ◽  
In Vitro Drug Release ◽  
Percentage Yield ◽  
Drug Entrapment Efficiency

The objective of the present investigation was to evaluate the entrapment efficiency of the anti-HIV drug, zidovudine, using natural gums and study the zidovudine release. Zidovudine-loaded microspheres were prepared by external ionotropic gelation technique. Sodium alginate in combination with guar gum or xanthan gums in different ratios were used. The microspheres of different core: coat ratios were formulated and evaluated for entrapment efficiency, particle size, percentage yield, swelling index, in vitro drug release and kinetic studies. Drug polymer compatibility studies were performed by Fourier Transform Infrared (FTIR) spectroscopy. The formulation was characterized by X-ray powder diffraction (XRD) and scanning electron Microscope (SEM). The zidovudine loaded microspheres have a particle diameter ranging approximately 450-779 μm. The FTIR showed compatibility between drug and excipients. Processing parameters (stirring speed, concentration of cross linking agent, volume of the processing medium on drug entrapment efficiency were optimized. F20 (1 g of sodium alginate and 0.150 g of guar gum) and F13 (1 g of sodium alginate, 0.250 g of xanthan gum) formulations showed better release (ANOVA, ˂0.05) profiles over a period of 12 h. Natural gums are biodegradable, safe, non-toxic and are used as release retardants and these can be extended to prepare microspheres of other drugs.

Preparation of ciprofloxacin-encapsulated poly-ε- caprolactone microcapsules by the solvent evaporation technique

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Marta Przybyslawska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Encapsulation Process ◽  
Evaporation Technique

Abstract The objective of this study was to prepare ciprofloxacin (CIP) encapsulated poly-ε-caprolactone (PCL) microcapsules by the single emulsion oilin- water (o/w) solvent evaporation method. The obtained microcapsules were characterized for size, morphology, drug loading and entrapment efficiency. The physical state of microcapsules was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TG). Storage stability, the in vitro drug release and mathematical modeling of drug release were also tested. It was found that obtained microcapsules had spherical shape and their size range was from 57.5 μm to 234.7 μm. The drug loading of microcapsules was from 1.72% to 11.02%. The optimal conditions of the encapsulation process include the drug/polymer ratio 2/1, using homogenizer for 5 min at 15000 rpm to disperse CIP in PCL solution and aqueous phase at pH 5.5. The results of CIP release study indicate that obtained microcapsules might be successfully used for designing sustained release dosage forms.

scholarly journals Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine

2015 ◽  
Vol 65 (1) ◽  
pp. 15-27 ◽  
Author(s):  
Marta Szekalska ◽  
Aleksandra Amelian ◽  
Katarzyna Winnicka
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Spray Drying ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Narrow Particle Size Distribution ◽  
In Vitro Drug Release ◽  
Adhesive Layers ◽  
First Order Kinetics

Abstract The present study is aimed at formulation of alginate (ALG) microspheres with ranitidine (RNT) by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers - gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9 %. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach

scholarly journals Preparation and In vitro Evaluation of Isoniazid-Containing Dex-HEMA-Co-PNIPAAm Nanogels

2015 ◽  
Vol 37 ◽  
pp. 55 ◽  
Author(s):  
Maryam Jafari ◽  
Babak Kaffashi
Keyword(s):  
Drug Loading ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Loading Capacity ◽  
In Vitro Drug Release ◽  
E Coli ◽  
Toxic Product ◽  
Good Biocompatibility ◽  
Characteristic Features

In this work, Dex-HEMA-Co-PNIPAAm nanogels containing Isoniazid antibiotic were made. Characteristic features of nanogels were studied by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS) and scanning electron microscopy (SEM). Drug loading capacity and entrapment efficiency were determined. In vitro drug release amount was estimated at room and body temperature. Biocompatibility of gels was investigated through cytotoxicity assay. Finally antimicrobial properties of synthesized gels were studied. It was shown from the experimental data that the nanogels size after drug loading increased about 1-2%. %Isoniazid loading and %entrapment efficiency were in the range of 15-22% and 37-48% respectively. After 10 days of degradation ca. 80% at 25ºC and ca. 90% at 37ºC of the nanogel structures were destructed. No significant toxic product produced while degradation and all nanogels depicted good biocompatibility. No antimicrobial features observed through the test condition against gram negative E Coli.

Folate conjugated solid lipid nanoparticle: formulation development, optimization and characterization

2021 ◽  
Vol 11 ◽  
Author(s):  
Vaibhav Rajoriya ◽  
Varsha Kashaw ◽  
Sushil Kumar Kashaw
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Release Study

Objective: The current paper represents the development, optimization, and characterization of paclitaxel-loaded folate conjugated solid lipid nanoparticles (FA-SLNs). Methods: The ligand (FA-SLNs) conjugated and non-conjugated SLNs (PTX-SLNs) were prepared by hot homogenization method. Both of the formulations (FA-SLNs and PTX-SLNs) were optimized with various parameters i.e. drug loading, stirring time, stirring speed, particle size, and polydispersity index, and characterized. The in-vitro drug release study was performed in different pH environments by using the dialysis bag method. The surface morphology and particle size were determined through scanning electron micorscopy and Transmission Electron Microscopy respectively, The SLNs formulations were also evaluated for the stability study. Result: The particle size of PTX-SLNs and FA-SLNs was determined and found to be 190.1±1.9 and 231.3±2.3 nm respectively. The surface morphology of the SLNs indicates that the prepared formulations are round-shaped and show smooth surfaces. The TEM study indicated that particles were in the range of 100-300 nm. The entrapment efficiency and drug loading capacity of FA-SLNs were found to be 79.42±1.6% and 17.3±1.9%, respectively. In-vitro drug release study data, stated that the optimum drug release was found in an acidic environment at pH 4.0, that showed 94.21% drug release after 16 hours and it proves that optimized formulation FA-SLNs will gave the sustained and better release in tumor tissue that owing acidic environment because of the angiogenesis process. Conclusion: In this research paper, different formulation parameters, found to influence fabrication of drug into Solid lipid nanoparticles, were optimized for high entrapment efficiency and drug loading. The most important parameters were drug:lipid ratio, drug:polymer ratio and lipid: surfactant ratio. Higher in-vitro drug release was observed in pH 4 as compared to the pH 7.4. These result data concludes that FA-SLNs formulation was successfully prepared, optimized and characterized.

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