scholarly journals FORMULATION AND OPTIMIZATION BY APPLYING 32 FULL FACTORIAL DESIGN OF MUCOADHESIVE MICROSPHERES OF NIFEDIPINE

2019 ◽  
pp. 321-327
Author(s):  
CHIMAN LAL ◽  
RAJEEV GARG ◽  
GHANSHYAM DAS GUPTA
Keyword(s):  
Research Work ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Microscopy Study ◽  
Electron Microscopy Study ◽  
Stability Study ◽  
Stirring Time ◽  
Drug Entrapment Efficiency ◽  
Full Factorial

Objective: The purpose of this research work is to formulate and optimize mucoadhesive microspheres of nifedipine using Carbopol 934P as mucoadhesive and ethyl cellulose as a carrier polymer for controlling the release of nifedipine. Methods: The emulsion solvent evaporation technique was used for the preparation of microspheres and the 32 full factorial designs were employed for optimization of microspheres. The developed microspheres were characterized for percent yield, entrapment efficiency, particle size, in vitro release study, percent mucoadhesion, surface morphology, and stability study. Results: Evaluating outcomes of preliminary batches indicated that 100 ml volume of processing medium, 5 h stirring time and 2% concentration of emulsifying agent were suitable for spherical, free-flowing microspheres and high percentage drug entrapment efficiency. The optimized batch exhibited 84.35% drug entrapment efficiency, 61.78% mucoadhesion and drug release were also sustained for more than 12 h. Scanning electron microscopy study revealed that produced microspheres were spherical in shape. Conclusion: Experimental responses of the optimized batch have close proximity with the predicted value and stability study of the optimized formulation proved the formulation is stable for a long period of time; hence, it is an excellent alternative over the conventional delivery system.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally

2020 ◽  
Vol 10 (1) ◽  
pp. 12-20
Author(s):  
Gaurav Tiwari ◽  
Ruchi Tiwari ◽  
Rachna Singh ◽  
Awani K. Rai
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Human Organ ◽  
Ethanol Injection ◽  
Release Studies ◽  
Junction Protein ◽  
Penetration Ability

Introduction: Transferosomes also known as ultra-deformable liposomes were introduced by Gregor Cevc in 1990. These are deformable vesicles that transport drug across the skin, which is the best route of drug delivery because skin is the largest human organ with 3 kg total weight and a surface area of 1.5-2.0 m2. Methods: Transferosomes are able to efficiently deliver low as well as high molecular weight drug across the skin in terms of quantity and depth. Various methods used for the preparation of transferosomes such as thin film hydration method, reverse phase evaporation method, vortex/sonication method, ethanol injection method and freeze thaw method. Results: The prepared transferosomal preparation will be evaluated for particle shape and size, entrapment efficiency, stability study, penetration ability and skin permeation study. In vitro release studies are to be performed using a specific dissolution medium. Conclusion: Ultra deformable liposomes can be used for delivery of different drugs e.g. analgesic, anesthetic, corticosteroids, anticancer, sex hormone, insulin, gap junction protein, and albumin.

scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF CURCUMIN LOADED JACKFRUIT SEED STARCH NANOPARTICLES

2020 ◽  
pp. 32-35
Author(s):  
JUNMONI NATH
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Infrared Studies ◽  
Drug Entrapment Efficiency ◽  
Starch Nanoparticles ◽  
Vitro Release

Objectives: To meet the above aim the following objectives are undertaken: (1) Isolation of starch from jackfruit seeds and formulation of curcumin loaded jackfruit seed starch nanoparticles (2) In vitro evaluations of the drug loaded nanoparticles Methods: Jackfruit seed starch nanoparticles were prepared by Nanoprecipitation technique. In this technique, jackfruit seed starch was mixed with curcumin and acetone solution using a magnetic stirrer at 600 rpm. To the above solution, water were added dropwise and stirred at room temperature until acetone was completely vaporized. Nanoparticles were separated by centrifugation at 4000 rpm after 40 min. Results: Particle size of prepared nanoparticle formulations was found to be 371 to 411.72 nm with PDI of 0.148 to 0.356. The maximum % drug entrapment was found to be 57.34 % with formulation F5. In vitro release studies showed sustained release of drug till 12 h. Conclusion: The prepared nanoparticles were evaluated for its particle size, drug entrapment efficiency, in vitro drug release study, and surface morphology studies by scanning electron microscopy. The results of Fourier transform infrared studies of 1:1 physical mixture of drug and excipients confirmed the absence of incompatibility. Thus, the study concludes that curcumin loaded jackfruit seed starch nanoparticles were developed successfully by nanoprecipitation, which is expected to enhance the oral bioavailability of curcumin.

scholarly journals DESIGN, FORMULATION AND EVALUATION OF LIPOSOME CONTAINING ISONIAZID

2018 ◽  
Vol 10 (2) ◽  
pp. 52 ◽  
Author(s):  
Akshay Singha Roy ◽  
Sudipta Das ◽  
Arnab Samanta
Keyword(s):  
In Vitro Release ◽  
Particle Diameter ◽  
Weight Ratio ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Skewed Distribution ◽  
Size Analysis ◽  
Scanning Calorimetry

Objective: The objective of the present study was to formulate and evaluate liposomes loaded with isoniazid.Methods: Liposome of isoniazid was made by thin layer film hydration method. L-α-phosphatidylcholine and cholesterol were used to make multiamellar vesicles. Six batches of liposomes were prepared based on the different weight ratio of L-α-phosphatidylcholine and cholesterol. Differential scanning calorimetry (DSC) study conducted to study in any incompatibility.Results: The prepared liposomes were evaluated by particle size analysis, entrapment efficiency, release study and stability study. Particle sizes were determined from the scanning electron microscopy (SEM) photographs. When particle frequencies were plotted against particle diameter in the histogram, it showed that F1 batch had a skewed distribution towards smaller liposomes while F6 shows a proper bell-shaped curve with a mean at 225 mm. The percentage entrapment efficiency was found to be 8.99 ± 0.15 to 4.19 ± 0.12 % respectively. From the release profile, it was seen that F1 batch was fastest and F6 was slowest to release the drug. The satisfactory batch F1 was packed in Eppendorf tube and stored at 4 °C temperature for one month. At the end of one month, the samples were analyzed for their physical properties, drug entrapment and in vitro release profile. The percentage release was found to be 96.5 ± 3.2 after 4 h.Conclusion: The F1 batch showed most promising results compared to other. No significant change was found during one month’s stability study of final batch (F1).

scholarly journals OPTIMIZATION AND CHARACTERIZATION OF DOXORUBICIN LOADED SOLID LIPID NANOSUSPENSION FOR NOSE TO BRAIN DELIVERY USING DESIGN EXPERT SOFTWARE

2021 ◽  
pp. 45-57
Author(s):  
VIRAG A. SHAH ◽  
JAYVADAN K. PATEL
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
High Speed ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
Solid Lipid ◽  
Stirring Time

Objective: The goal of the current study was to investigate the possible use of solid lipid nanosuspension (SLNs) as a drug delivery method to boost doxorubicin (DOX) brain-targeting performance after intranasal (i. n.) administration.  Methods: 33 factorial design was applied for optimization by using lipid concentration, surfactant concentration, and High-speed homogenizer (HSH) stirring time as dependent variables, and their effect was observed on particles size, Polydispersity index (PDI), and entrapment efficiency.  Results: With the composition of Compritol® 888 ATO (4.6 % w/v), tween 80 (1.9 % w/v), and HSH stirring time, the optimized formula DOX-SLNs prepared (10 min). Particle size, PDI, zeta potential, entrapment efficiency, percent in vitro release were found to be 167.47±6.09 nm, 0.23±0.02, 24.1 mV, 75.3±2.79, and 89.35±3.27 percent in 24 h, respectively, for optimized formulation (V-O). No major changes in particle size, zeta potential, and entrapping efficiency were found in the stability studies at 4±2 °C (refrigerator) and 25±2 °C/60±5% RH up to 3 mo.  Conclusion: Following the non-invasive nose-to-brain drug delivery, which is a promising therapeutic strategy, the positive findings confirmed the current optimized DOX-loaded SLNs formulation.

scholarly journals Design and Optimization of Novel Vaginal Microsphere Gel of Clotrimazole

2021 ◽  
Vol 22 (2) ◽  
Author(s):  
Snehal Bhabad ◽  
Snehal Bhabad . ◽  
Snehal Bhabad .
Keyword(s):  
Entrapment Efficiency ◽  
Stability Study ◽  
Vaginal Candidiasis ◽  
Vaginal Fluid ◽  
In Vitro Drug Release ◽  
Design And Optimization ◽  
Microsphere Preparation ◽  
Novel Drug ◽  
Full Factorial

The objective of the study was to develop and evaluate sustained release microsphere gel for the drug clotrimazole to be administered through the vaginal route. The effect of polymer ethylcellulose and carbopol 934 on entrapment efficiency and diffusion behavior were investigated respectively. A 32 full-factorial design was used to optimize the formulation of Microsphere gel. Microspheres were characterized by SEM, FTIR, Entrapment efficiency, and particle size. Gels were evaluated for in-vitro drug release in simulated vaginal fluid. The microsphere loaded with clotrimazole in bioadhesive carbopol gel formulation was evaluated for various physicochemical studies and was found to be satisfactory. The rheological profile shows the gel formation at desired condition. It is evaluated for spreadability, drug content, In-vitro drug diffusion, stability study, and bioadhesive study. It may be concluded that spray drying is a suitable method for microsphere preparation and microsphere gel can be used as a novel drug delivery system to prolonge release of clotrimazole for vaginal candidiasis.

scholarly journals TRIVALENT ION CROSS-LINKED AND ACETALATED GELLAN GUM MICROSPHERES OF GLIMEPIRIDE

2020 ◽  
pp. 66-68
Author(s):  
SUDIPTA DAS ◽  
RIMI DEY
Keyword(s):  
In Vitro Release ◽  
Microscopic Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Gellan Gum ◽  
Long Term Stability ◽  
Vitro Release

Objectives: A novel formulation was developed with glimepiride loaded trivalent ion Al+3 cross-linked and acetalated gellan gum microspheres. Methods: The glimepiride loaded microspheres were formulated using sodium alginate and gellan gum. Cross-linking agents used for the microspheres were aluminum chloride (AlCl3) and glutaraldehyde (GA). The evaluation processes of prepared microspheres were carried out by in-vitro release study, swelling index, microscopic analysis, and entrapment efficiency. Results: All the formulations show good entrapment efficiency and the maximum entrapment 84.6% was governed by the formulation (F3) cross-linked by AlCl3 and GA and their obtained mean particle size were 12.46±3.21 μm. Release profile of the formulations revealed the sustained design of the drug, particularly this formulation (F3), releasing approximately 40% over 4 h. Conclusions: From this experiment, it can be accustomed that F3 possesses higher standard formulation than the rest due to good release profile and entrapment efficiency. Therefore, the long term stability study is required for future development of this formulation.

scholarly journals Preparation and Characterization of Nano Structured Lipid Carriers for Ocular Bacterial Infection

2021 ◽  
pp. 8-23
Author(s):  
Shubhangi Aher ◽  
Ravindra Pal Singh ◽  
Manish Kumar
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tolerance Test ◽  
Stability Study ◽  
Scanning Calorimetry ◽  
Bacterial Conjunctivitis ◽  
Pure Drug

The problem of bacterial conjunctivitis has dramatically increased in recent years due increased pollution and modern lifestyle. The present study was focused to fabricate Sparfloxacin loaded nanostructured lipid carriers (Spar-NLCs) for ophthalmic application to improve ocular penetration of drug and give sustained release of drug to reduce dosing frequency and toxic effect of drug associated with ocular membrane. A regular two-level factorial design was used to optimize the formulation parameters that are significantly affecting the formulation attributes. Spar-NLCs with particle size 171.1 ± 11 nm, zeta potential -49 ± 6.47 mV, entrapment efficiency 89.5 ± 5% and spherical in shape was obtained. Besides this, FTIR spectroscopy, differential scanning calorimetry, and transmission electron microscopy results suggest that the drug is successfully incorporated in NLC and has excellent compatibility with the excipients. In vitro release study follows Korsmeyer peppas model and suggests that 81.35 ± 6.2% release of drug from Spar-NLCs in 12 hours. The result of ex-vivo permeation study demonstrated 349.75 ± 7.3 µg/cm2 of permeation of drug, 44.482 µg cm-2 hr -1 of flux, and 0.1482 cm hr-1 of permeability coefficient which is 1.7 folds higher than pure drug suspension. The antimicrobial activity of Spar-NLCs was better than the pure drug suspension and equivalent to the marketed formulation. Spar-NLC formulation did not showed any ocular damage, swelling, and redness in in -vivo Draize test. The ocular tolerance test (HET-CAM test) also suggests that the Spar-NLC formulation and its excipients were nonirritant to the ocular tissues. The formulation was found to be stable over the three month of stability study. Therefore, this work strongly suggest that Spar-NLCs has higher penetration and extended release of drug which can be effectively used in prevention of bacterial conjunctivitis.

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