Development of Rifampicin Nanoparticles by 32 Factorial Design

2010 ◽  
Vol 3 (3) ◽  
pp. 1085-1091
Author(s):  
Gambhire Makarand ◽  
Vaishali Gambhire ◽  
Bhalekar Mangesh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
Chemical Interaction ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Sustained Drug Release ◽  
32 Factorial Design

The preparation and physico-chemical evaluation of rifam-picinloaded poly-(lactic-co-glycolic) acid (PLGA) nanoparticles as per 32 Factorial Design are presented. PLGA (X1) and PVA (Polyvinyl alcohol) solution (X2) as a stabilizing agent were used as independent variables where Particle size (PS) (Y1), Entrapment Efficiency (EE) (Y2) and % Drug Release at 12th h (REL)(Y3) were taken as dependant variables. Rifampicin nanoparticles were prepared by multiple emulsion solvent evaporation method. The results showed the method as reproducible, easy and efficient is the entrapment of drug as well as formation of spherical nanoparticles. Effect of polymer concentration was also evaluated with respect to their % drug entrapment efficiency. The in vitro release studies indicated the rifampicin-loaded PLGA nanoparticles provide sustained drug release over a period of 12h. The optimum batch was R3 which shown particle size 326 nm, 61.70 % EE and 57. 50% drug release at 12th h. Infrared spectroscopy analysis revealed that there was no known chemical interaction between drug and polymer. Hence, this investigation demonstrated the potential of the experimental design in understanding the effect of the formulation variables on the quality of rifampicin nanoparticles.

scholarly journals Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Entrapment Efficiency ◽  
Pulmonary Drug Delivery ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

DEVELOPMENT OF GASTRO-RETENTIVE FLOATING MICROSPHERES OF ONDANSETRON HYDROCHLORIDE

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (08) ◽  
pp. 22-27
Author(s):  
S. G Bandbe ◽  
◽  
K Dixit ◽  
G Laghate ◽  
R. B. Athawale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Ondansetron Hydrochloride ◽  
Percentage Yield ◽  
Gastro Retentive

Ondansetron hydrochloride (OND) is indicated for prevention of nausea and vomiting during chemotherapy. Due to its insolubility in intestinal pH, it is absorbed only in the stomach. In the present study, an attempt was made to increase gastric retention time of ondansetron hydrochloride by preparing its floating microspheres by solvent evaporation method with ethyl cellulose (EC) and hydroxypropylmethylcellulose (HPMC). Microspheres were characterized for percentage yield, particle size, surface morphology, floating behaviour, entrapment efficiency and in vitro release. Polymer ratio and stirring speed seemed to have significant impact on size, entrapment efficiency, floating time and release profile. Hydroxypropylmethylcellulose: ethyl cellulose in the ratio 1: 3, gave most suitable buoyancy and drug release. By increasing polymer concentration, the mean particle size of microspheres increased while drug release rate decreased. Developed formulation of ondansetron hydrochloride can be used for prolonging its retention in the stomach for at least 12 hrs, thereby improving bioavailability and patient compliance.

scholarly journals FORMULATION AND CHARACTERIZATION OF MICROSPHERES OF NITAZOXANIDE BY CHEMICAL CROSSLINKING METHOD

2018 ◽  
Vol 8 (5) ◽  
pp. 190-199
Author(s):  
A K Sachan ◽  
A Gupta ◽  
K Kumari ◽  
A Ansari
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Drug Delivery ◽  
First Order Kinetics ◽  
Drug Entrapment Efficiency

The work investigated the design and evaluation of microspheres of Nitazoxanide by Ionotropic gelation technique met. 32 Factorial designs were used and concentration of polymer carbopol-934 (X1) and Ethyl cellulose (X2) were selected as the independent variables. The surface morphology study by SEM indicated that microspheres were spherical with smooth surface. There was no interaction between the drug and polymers, as studied by FTIR study. The prepared microspheres were characterized by entrapment efficiency, particle size micromeritic properties. It was observed that on increasing polymer concentration of formulations, % yield, the entrapment efficiency and particle size were increased whereas % drug release decreased. The In Vitro release study was done using U.S.P. dissolution rate basket type apparatus in phosphate buffer pH 7.4 for 10 hr. It shows that on increasing polymer concentration the drug release of all formulations was gradually decreased. In Vitro mucoadhesion study depicts that as the polymer concentration increased, mucoadhesive nature of the formulation was also increased. The microspheres of NTZ (formulation F9) showed best results due to highest drug entrapment efficiency (85.50%), and percentage drug release after 10.0 hr. was 50.25%. The rate of release followed First order kinetics. The microspheres exhibits good mucoadhesive properties in  in- vitro wash-off test at pH 7.4 (Intestinal pH) than pH 1.2 (gastric pH),because the drug was completely absorbed in Gastrointestinal tract, Therefore, it can be concluded that Nitazoxanide Loaded algino-carbopol-934 microspheres can be formulated for sustained drug delivery of Nitazoxanide used in Chronic Hipatitis-C. Keywords: Mucoadhesive microspheres, Nitazoxanide, Carbopol-934, Ethyl cellulose, Sodium Alginate, Factorial design.

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 FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

2021 ◽  
pp. 272-277
Author(s):  
DIVYA ◽  
INDERBIR SINGH ◽  
UPENDRA NAGAICH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Seborrheic Dermatitis ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Flow Index ◽  
In Vitro Evaluation

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery.

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 Effect of A 2-HP-β-Cyclodextrin Formulation on the Biological Transport and Delivery of Chemotherapeutic PLGA Nanoparticles

2020 ◽  
Author(s):  
Kangyu Zheng ◽  
Zeju Huang ◽  
Jiaying Huang ◽  
Xiangmei Liu ◽  
JUNFENG BAN ◽  
...  
Keyword(s):  
Drug Release ◽  
Cellular Uptake ◽  
Entrapment Efficiency ◽  
Plga Nanoparticles ◽  
Human Lung Cancer ◽  
Pharmacokinetic Analysis ◽  
Biological Transport ◽  
Sustained Drug Release

Abstract Background: The aim of this work was to develop a novel and feasible modification strategy by utilizing the supramolecular effect of 2-hydroxypropyl-beta-cyclodexrin (2-HP-β-CD) for enhancing the biological transport efficiency of paclitaxel (PTX)-loaded poly(lactide-co-glycolide)(PLGA) nanoparticles.Methods: PTX-loaded 2-HP-β-CD-modified PLGA nanoparticles (2-HP-β-CD/PLGA NPs) were prepared using the modified emulsion method. Nano-characteristics, drug release behavior, in vitro cytotoxicity, cellular uptake profiles and in vivo bio-behavior of the nanoparticles were then characterized. Results: Compared with the plain PLGA NPs, 2-HP-β-CD/PLGA NPs exhibited smaller particle sizes (151.03±1.36 nm), increased entrapment efficiency (~49.12% increase) and sustained drug release. When added to A549 human lung cancer cells, compared with PLGA NPs, 2-HP-β-CD/PLGA NPs exhibited higher cytotoxicity in MTT assays and improved cellular uptake efficiency. Pharmacokinetic analysis showed that the AUC value of 2-HP-β-CD/PLGA NPs was 2.4-fold higher than commercial Taxol® and 1.7-fold higher than plain PLGA NPs. In biodistribution assays, 2-HP-β-CD/PLGA NPs exhibited excellent stability in the circulation.Conclusions: The results of this study suggest that formulation contains 2-HP-β-CD can prolong PTX release, enhance drug transpot efficiency and serve as a potential tumor targeting system for PTX.

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.

Formulation Development of Aceclofenac Loaded Nanosupension by Three Square (32) Factorial Design

2012 ◽  
Vol 4 (4) ◽  
pp. 1575-1583
Author(s):  
Atul A Patak ◽  
Jorwekar, P ◽  
P D Chaudhari
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Factorial Design ◽  
In Vivo Studies ◽  
Differential Scanning Calorimetric ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Calorimetric Analysis ◽  
32 Factorial Design

In the present study, aceclofenac loaded polymeric nanosuspension were formulated and evaluated.  Aceclofenac is a potent analgesic under BCS Class II. Due to the need for its frequent dosing, aceclofenac is an ideal candidate for sustained or controlled drug delivery. For optimization of prepared formulation, the three square (32) factorial design was used.  Tween 80 (X1) and combination of Eudragit RL 100 and RS 100 (X2) were used as independent variables and particle size (Y1), entrapment efficiency (Y2), and Percent drug release (Y3) were taken as dependent variables. The formulations were evaluated for particle size, zeta potential and drug entrapment. The in vitro drug release profile supports nanosuspension form to be used as a sustained release vehicle for aceclofenac. The formulation was characterized by differential scanning calorimetric analysis, in vivo studies and stability testing.

scholarly journals Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

2021 ◽  
Author(s):  
Cheran K ◽  
Udaykumar B Bolmal ◽  
Archana S Patil ◽  
Umashri A Kokatanur ◽  
Rajashree S Masareddy
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Gastro Retentive

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

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