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.

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.

scholarly journals Development of Sustained Release Baricitinib Loaded Lipid-Polymer Hybrid Nanoparticles with Improved Oral Bioavailability

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 168
Author(s):  
Md. Khalid Anwer ◽  
Essam A. Ali ◽  
Muzaffar Iqbal ◽  
Mohammed Muqtader Ahmed ◽  
Mohammed F. Aldawsari ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Janus Kinase ◽  
Hybrid Nanoparticles ◽  
Polymer Hybrid ◽  
Vitro Release

Baricitinib (BTB) is an orally administered Janus kinase inhibitor, therapeutically used for the treatment of rheumatoid arthritis. Recently it has also been approved for the treatment of COVID-19 infection. In this study, four different BTB-loaded lipids (stearin)-polymer (Poly(d,l-lactide-co-glycolide)) hybrid nanoparticles (B-PLN1 to B-PLN4) were prepared by the single-step nanoprecipitation method. Next, they were characterised in terms of physicochemical properties such as particle size, zeta potential (ζP), polydispersity index (PDI), entrapment efficiency (EE) and drug loading (DL). Based on preliminary evaluation, the B-PLN4 was regarded as the optimised formulation with particle size (272 ± 7.6 nm), PDI (0.225), ζP (−36.5 ± 3.1 mV), %EE (71.6 ± 1.5%) and %DL (2.87 ± 0.42%). This formulation (B-PLN4) was further assessed concerning morphology, in vitro release, and in vivo pharmacokinetic studies in rats. The in vitro release profile exhibited a sustained release pattern well-fitted by the Korsmeyer–Peppas kinetic model (R2 = 0.879). The in vivo pharmacokinetic data showed an enhancement (2.92 times more) in bioavailability in comparison to the normal suspension of pure BTB. These data concluded that the formulated lipid-polymer hybrid nanoparticles could be a promising drug delivery option to enhance the bioavailability of BTB. Overall, this study provides a scientific basis for future studies on the entrapment efficiency of lipid-polymer hybrid systems as promising carriers for overcoming pharmacokinetic limitations.

scholarly journals Formulation and Evaluation of Parenteral Sustained Release Microspheres of Diclofenac Sodium

2003 ◽  
Vol 71 (2) ◽  
pp. 101-111
Author(s):  
C. Sajeev ◽  
R. Archna ◽  
V. Gupta ◽  
A. Sobti ◽  
R. Saha
Keyword(s):  
Sustained Release ◽  
Response Time ◽  
Diclofenac Sodium ◽  
In Vitro Release ◽  
Tail Flick ◽  
Duration Of Action ◽  
Sustained Release Formulation ◽  
Vitro Release

The aim of this study was to formulate and evaluate microsphere based depot type parenteral sustained release formulation of diclofenac sodium (DFS). Drug was formulated in the form of microspheres, using varying proportion of ethylcellulose (EC) as the retardant material to extend the release, by phase separation-coacervation technique. The in vitro release pattern of the designed formulations was studied using modified Franz diffusion cell. In vivo pharmacodynamic study was carried out by determining the index of analgesia (increase in response time to thermal stress as percentage of basal response time). Tail flick method was employed to measure both the degree of analgesia and its duration of action. The prepared microspheres were white, free flowing, and spherical in shape with a mean particle size of 50 μm. In vitro release study of the micro-spheres in aqueous media was found to extend the release of DFS beyond 24 hours with DFS and EC ratio 1:3. The plot of log percentage remaining to be released vs. time gave a linear relationship indicating first-order release kinetics. The in vitro release rate constant (Kr) for different microspheres varied between 0.1448 hr-1 and 0.0256 hr-1. A good correlation was obtained between K, and proportion of EC in the microspheres. In vivo pharmacodynamic studies indicated that the duration of analgesic action is prolonged beyond 24 hrs in case of microsphere products of 1:3 ratio of DFS to EC, whereas administration of marketed parenteral preparation showed activity only up to 11hrs. Also, a good correlation was obtained between analgesic activity in vivo and cumulative percentage of drug release from the formulations.

scholarly journals DEVELOPMENT AND COMPARISON OF ORALLY INHALABLE SUSTAINED RELEASE FORMULATIONS FOR THREE RESPIRATORY DRUGS FOR ASTHMA

2016 ◽  
Vol 12 (25) ◽  
pp. 5679-5699
Author(s):  
K.Sathish Kumar ◽  
C. Kumaresan ◽  
R. Anantharaj
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Solvent Evaporation Method ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Montelukast Sodium ◽  
Ambroxol Hydrochloride ◽  
Vitro Release ◽  
Respiratory Drugs

The present work was designed to develop and compare orally inhalable sustained release formulation for salbutamol sulphate (SS), ambroxol hydrochloride (AH) and montelukast sodium (MS).The emulsion solvent evaporation method was used to prepare microparticles with the polymers. The prepared polymer encapsulated microparticles were blended with carrier inhalable lactose and filled in size 3 hard empty gelatin capsule. Formulations T1-T9 were prepared with 1:1 ratio of PLGA (50:50), PLGA (75:25) and Eudragit RS100. The formulation T1 prepared with SS:PLGA (50:50) produces best result when compared with other formulations T2-T9. Formulation T1 gives in vitro release 91.23% at 12 h and having particle size of microparticles (D0.5 µm) 1.94±0.6 and respiratory fraction 34.9± 2.59 %.

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.

Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach

2020 ◽  
Vol 10 (2) ◽  
pp. 149-158
Author(s):  
Guilherme A.G. Martins ◽  
Fabio S. Murakami ◽  
Mauro S. Oliveira ◽  
Ana F. Furian ◽  
Helen Treichel ◽  
...  
Keyword(s):  
Quality By Design ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
In Vivo Studies ◽  
Mean Size ◽  
Release Study ◽  
Vitro Release

Objective: Atorvastatin (ATV) is effective in reducing total cholesterol and low-density lipoprotein levels. Furthermore, it produces pleiotropic effects in neurodegenerative conditions such as Parkinson's, Alzheimer's, and epilepsy. However, due to the effective defense system of the central nervous system (CNS), the development of new medicines for clinical conditions has proven difficult. In this context, nanotechnology was applied as a promising solution to promote drug vectorization to the brain. Methods: The solvent emulsification-diffusion method was used to develop nanoparticles (NPs) based on polylactic acid and coated with polysorbate 80 containing ATV. Quality-by-Design (QbD) was used in the optimization of nanoparticles production through the application of the experimental design Box-Behnken Design. Results: After optimizing the independent factors including sonication time, surfactant concentration and surfactant volume, the NPs presented physicochemical characteristics such as entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. Conclusion: The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies. The physicochemical characteristics included entrapment efficiency of 86.4 ± 2.4%, mean size of 225.2 ± 4.8 nm, and zeta potential of -14.4 ± 0.36 mV. In the in vitro release study, approximately 20% of the encapsulated ATV was released. The application of QbD was very useful in demonstrating its applicability in the nanotechnological pharmaceutical area for controlling and predicting the influence of the variables in the production of NPs. The NPs developed in this study presented adequate physicochemical characteristics, which is promising for future in vivo studies.

scholarly journals Biodegradable microparticulate drug delivery system of diltiazem HCl

2012 ◽  
Vol 48 (4) ◽  
pp. 699-709 ◽  
Author(s):  
Manish Kumar Gupta ◽  
Deepak Prakash ◽  
Brahmeshwar Mishra
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Particle Size ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Diltiazem Hcl ◽  
Vitro Release ◽  
Scanning Electron

The efficacy of a drug in a specific application requires the maintenance of appropriate drug blood level concentration during a prolonged period of time. Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development. The objective of this work is to prepare and evaluate diltiazem HCl loaded albumin microparticles using a factorial design. Albumin (natural polymer) microparticles were prepared by emulsion heat-stabilization method. Selected formulations were characterized for their entrapment efficiency, particle size, surface morphology, and release behavior. Analysis of variance for entrapment efficiency indicates that entrapment efficiency is best fitted to a response surface linear model. Surface morphology was studied by scanning electron microscopy. Scanning electron microscopy of the microparticles revealed a spherical, nonporous and uniform appearance, with a smooth surface. The geometric mean diameter of the microparticles was found to be 2-9 µm, which more than 75% were below 3.5 µm and drug incorporation efficiency of 59.74 to 72.48% (w/w). In vitro release profile for formulations containing diltiazem HCl loaded BSA microparticles with heat stabilization technique shows slow controlled the release of the drug up to 24 hours. The release pattern was biphasic, characterized by an initial burst effect followed by a slow release. All selected microparticles exhibited a prolonged release for almost 24 hours. On comparing regression-coefficient (r²) values for Hixson Crowel, Higuchi and Peppas kinetic models, different batches of microparticles showed Fickian, non-Fickian, and diffusion kinetics. The release mechanism was regulated by D:P ratio. From the statistical analysis it was observed that as the drug:polymer (D:P) ratio increased, there was a significant increase in the encapsulation efficiency. Based on the particle size, entrapment efficiency and physical appearance, DTM-3 formulations were selected for in vivo release study and stability study. The in vivo result of drug loaded microparticles showed preferential drug targeting to liver followed by lungs, kidneys and spleen. Stability studies showed that maximum drug content and closest in vitro release to initial data were found in the formulation stored at 4 ºC. In present study, diltiazem HCl loaded BSA microparticles were prepared and targeted to various organs to satisfactory level and were found to be stable at 4 ºC.

scholarly journals FORMULATION AND EVALUATION OF ALLOPURINOL LOADED CHITOSAN NANOPARTICLES

2019 ◽  
pp. 49-52 ◽  
Author(s):  
Gurpreet Kandav ◽  
D.c. Bhatt ◽  
Deepak Kumar Jindal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Polydispersity Index ◽  
Sustained Release Formulation

Objective: The objective of the present investigation was to fabricate and characterize allopurinol loaded chitosan nanoparticles (A-CNPs) for sustained release of drug. Methods: The allopurinol loaded chitosan nanoparticles were successfully prepared by employing the ionotropic gelation method. Further, particle size (PS), polydispersity index (PDI), zeta potential (ZP), Differential Scanning Calorimetry (DSC), entrapment efficiency (EE), Transmission Electron Microscopy (TEM), in vitro drug release, X-Ray Diffraction (XRD) and Fourier transform infrared (FTIR) were used for evaluating formulated A-CNPs Results: A-CNPs was successfully prepared and the particle size, polydispersity index, ZP and entrapment efficiency were found to be 375.3±10.1 nm, 0.362±0.01 and 32.5±2.7 mV and 52.56±0.10% respectively. In vitro release profile of A-CNPs showed sustained release and Higuchi model was found to be best fit for drug release kinetics. FTIR study depicted no chemical interaction between pure drug allopurinol (AL) and other excipients. Conclusion: The sustained release formulation of allopurinol was successfully prepared using HMW chitosan and evaluated for different parameters.

scholarly journals DEVELOPMENT AND IN-VITRO CHARACTERISATION OF CHITOSAN LOADED PACLITAXEL NANOPARTICLE

2016 ◽  
Vol 9 (9) ◽  
pp. 145 ◽  
Author(s):  
Tumpa Sarkar ◽  
Abdul Baquee Ahmed
Keyword(s):  
Particle Size ◽  
High Speed ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Ionic Crosslinking ◽  
Glutaraldehyde Solution ◽  
Drug Entrapment Efficiency ◽  
Vitro Release

ABSTRACTObjectives: To meet the above aim the following objectives are undertaken: (1) Preparation of paclitaxel (PTX) loaded nanoparticles by differenttechniques, (2) In-vitro evaluations of the drug loaded nanoparticles and selection of optimized batch.Methods: PTX loaded chitosan nanoparticles were prepared by Ionic-crosslinking technique. In this technique, chitosan was dissolved in 0.25%v/vacetic acid solution. To this above solution 0.84%v/v, glutaraldehyde solution was added dropwise under high-speed homogenizer at 17000 rpm for1 hr.Result: Particle size of prepared nanoparticle formulations was found to be 345.175±5.66-815.125±8.355 nm with low PDI between 0.456. Themaximum entrapment of drug was found to be 88.57±2.533% with formulation F5. In-vitro release studies of the F5 formulation showed 57.8±1.735%release of drug after 24 hrs.Conclusion: The prepared nanoparticles were evaluated for its particle size, zeta potential, 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 andexcipients confirmed the absence of incompatibility. Thus, the study concludes that PTX loaded nanoparticles were developed successfully by ioniccrosslinking method, which is expected to enhance the oral bioavailability of PTX.Keywords: Paclitaxel, Nanoparticles, Chitosan, Ionic-crosslinking, In-vitro release.

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