scholarly journals SUSTAINED RELEASE MICROBEADS OF RITONAVIR: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 189-198
Author(s):  
D. NAGASAMY VENKATESH ◽  
S. SHASHI KUMAR ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Drug Entrapment Efficiency ◽  
Pure Drug

Objective: The main aim of the present investigation was to develop sustained release microbeads of ritonavir that has a shorter half-life (3-5 h) and requires twice a day administration. These formulations exhibit a sustained release of ritonavir that would expect to improve the therapy, better drug utilization, and patient compliance. Methods: Gellan-chitosan and calcium chloride reinforced beads of ritonavir were prepared by ionotropic gelation method employing different concentrations of gellan, chitosan, calcium chloride and drug. The prepared beads were evaluated for various physicochemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infrared spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo bioavailability studies. Results: From the results, formulation GC-II exhibited higher drug entrapment efficiency (79.65±0.012), higher swelling index, sustained drug release over a period of 24 h, increased oral bioavailability (2.07 times higher than that of pure drug) and decreased elimination rate (2.15 times lesser for ritonavir microbeads) with prolonged elimination half-life (2.15 times more than pure drug) as compared to pure drug. Conclusion: Ritonavir microbeads have demonstrated as a better delivery system for the sustained release of the drug; which may in turn circumvent the drawbacks associated with the conventional therapy.

scholarly journals FORMULATION AND CHARACTERISATION OF SUSTAINED RELEASE MICROBEADS LOADED WITH ZALTOPROFEN

2019 ◽  
pp. 173-180
Author(s):  
H. C. KIRAN ◽  
DHANDAPANI NAGASAMY VENKATESH ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Calcium Chloride ◽  
Oral Bioavailability ◽  
Half Life ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Drug Entrapment Efficiency

Objective: The main aim of the present investigation was to formulate and evaluate microbeads of zaltoprofen. Zaltoprofen, a BCS class II drug used in the treatment of rheumatoid arthritis. Zaltoprofen has a shorter half-life of 2.8 h, and it is administered at a dose of 80 mg thrice a day. By encapsulating the drug into microbeads, it is expected that the release of the drug would be prolonged and thereby, it reduces the frequency of administration and better patient compliance may be improved. Methods: Gellan-chitosan and calcium chloride beads of zaltoprofen were prepared employing ionotropic gelation method using different concentrations of gellan, chitosan, calcium chloride and zaltoprofen. The microbeads were evaluated for its various Physico-chemical parameters such as particle size determination, drug entrapment efficiency, infrared spectroscopy study, differential scanning calorimetry, X-ray diffraction analysis, scanning electron microscopy, in vitro drug release study and in vivo oral bioavailability studies. Results: The results suggested that the batch FG-II exhibited higher drug entrapment efficiency (72.42±0.013), a sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an enhanced oral bioavailability (2.4 times higher than that of pure drug), lower elimination rate (1.14 times lesser for the drug in microbeads) with prolonged elimination half-life (2.561 times higher than pure zaltoprofen). Conclusion: Zaltoprofen entrapped microbeads demonstrated as a better delivery system for the sustained release of drug and also to circumvent the drawbacks associated with conventional therapy.

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.

scholarly journals ENHANCED ORAL BIOAVAILABILITY OF TENOFOVIR FROM IONOTROPICALLY GELLED MICROBEADS

2019 ◽  
pp. 242-250
Author(s):  
DHANDAPANI NAGASAMY VENKATESH ◽  
PREETY RAO ◽  
RAMAN RAJESHKUMAR
Keyword(s):  
Drug Release ◽  
Calcium Chloride ◽  
Oral Bioavailability ◽  
Elimination Rate ◽  
Entrapment Efficiency ◽  
Dissolution Profile ◽  
Class Iii ◽  
Sustained Drug Release ◽  
Scanning Calorimetry ◽  
Drug Entrapment Efficiency

Objective: The main objective of the present investigation was to develop microbeads of tenofovir. Tenofovir, a BCS class III drug has a poor bioavailability of 25%, and it is administered 300 mg once a day. By incorporating the drug into a microparticulate carrier, it is expected that the dissolution profile and the oral bioavailability may be increased. Methods: Reinforced gellan-chitosan and calcium chloride beads of tenofovir were prepared by ionotropic gelation method employing various different concentrations of gellan, chitosan, calcium chloride and tenofovir. The beads were evaluated for various physico-chemical parameters such as particle size determination, drug entrapment efficiency, swelling studies, infra red spectroscopy study, differential scanning calorimetry, x-ray diffraction analysis, scanning electron microscopy, in vitro drug release study, cytotoxicity study and in vivo oral bioavailability studies. Results: From the results, it can be concluded that the formulation TB-III exhibited higher drug entrapment efficiency (46.09±0.21), a higher swelling index, sustained drug release for a period of 24 h. The pharmacokinetic profile of the drug from microbeads exhibited an increased oral bioavailability (1.25 times higher than that of pure drug), decreased elimination rate (1.32 times lesser for drug in microbeads) with prolonged elimination half-life (1.32 times higher than pure tenofovir). Conclusion: Tenofovir loaded microbeads demonstrated as a better delivery system for the modified release of drug and also to navigate the drawbacks associated with the conventional therapy.

Formulation and evaluation of sustained release saxagliptin microspheres by ionotropic gelation method

2017 ◽  
Vol 6 (03) ◽  
pp. 5328
Author(s):  
Madhuri Latha Thadanki*
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Release Kinetic ◽  
Flow Properties ◽  
Ionotropic Gelation ◽  
Drug Entrapment Efficiency

The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of an antidiabetic agent, saxagliptin. Saxagliptin microspheres were formulated using sodium alginate as the controlled release polymer by ionotropic gelation technique. The polymer sodium alginate alone and along with different coating polymers like pectin, ethyl cellulose was used in different ratios (1:1,1:1.5, 1:2 ) to formulate batches F1 to F9. The resulting microspheres were evaluated for particle size, densities, flow properties, morphology, recovery yield, drug content, drug entrapment efficiency and in vitro drug release behavior. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. The drug entrapment efficiency obtained in the range 70.4% to 95.2%.Among different formulations, the fabricated microspheres of batch F3 had shown the optimum percent drug encapsulation of microspheres and the sustained release of the saxagliptin for about 9 h. In vitro study showed that drug release slowly increases as the pH of the medium is increased. Release pattern of saxagliptin from microspheres of batch F3 followed Higuchi model and zero-order release kinetic model. The value of ‘n’ was found to be 0.867. The data obtained thus suggest that a microparticulate system can be successfully designed for sustained delivery of saxagliptin and to improve dosage form characteristics for easy formulation.

scholarly journals Preparation and Release Profiles in Vitro/Vivo of Galantamine Pamoate Loaded Poly (Lactideco-Glycolide) (PLGA) Microspheres

2021 ◽  
Vol 11 ◽  
Author(s):  
Liping Du ◽  
Shankui Liu ◽  
Guizhou Hao ◽  
Li Zhang ◽  
Miaomiao Zhou ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Solvent Evaporation Method ◽  
Sustained Drug Release ◽  
Water Emulsion ◽  
Oil Water

Patient’s poor compliance and the high risk of toxic effects limit the clinical use of galantamine hydrobromide. To overcome these drawbacks, the sustained-release galantamine pamoate microspheres (GLT-PM-MS) were successfully developed using an oil/water emulsion solvent evaporation method in this study. Physicochemical properties of GLT-PM-MS were carefully characterized, and the in vitro and in vivo drug release behaviors were well studied. Results showed that the morphology of optimized microspheres were spherical with smooth surfaces and core-shell interior structure. Mean particle size, drug loading and entrapment efficiency were 75.23 ± 1.79 μm, 28.01 ± 0.81% and 87.12 ± 2.71%, respectively. The developed GLT-PM-MS were found to have a sustained release for about 24 days in vitro and the plasma drug concentration remained stable for 17 days in rats. These results indicated that GLT-PM-MS could achieve the sustained drug release purpose and be used in clinical trial.

SUSTAINED RELEASE MULTIPARTICULATE GASTRORETENTIVE DELIVERY SYSTEM OF CINNARIZINE

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (07) ◽  
pp. 31-38
Author(s):  
Gurudev Kruthi ◽  
◽  
B. V. Basavaraj ◽  
S. Bharath ◽  
R. Deveswaran ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Delivery System ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Ir Studies ◽  
Sustained Drug Delivery ◽  
Release Studies ◽  
Drug Entrapment Efficiency

The main aim of the present work was to formulate and evaluate sustained release multiparticulate gastroretentive delivery system of cinnarizine. The microspheres were prepared by solvent evaporation method by using Eudragit RS 100 as a polymer in varying ratios. The prepared microspheres were evaluated for drug – polymer compatibility studies, micromeritic properties, drug entrapment efficiency, in vitro buoyancy and drug release studies. The mean particle size increased with increase in polymer concentration, ranging between 60.33 μm to 144.88 μm. FT IR studies showed that the drug and polymer were compatible with each other. The entrapment efficiency decreased with increase in the polymer concentration with values of 50%, 33.3% and 25% respectively. The microspheres floated upto 9 h over the surface of the gastric buffer medium and the buoyancy percentage was found to be in the range of 64.3 – 76.2%. In vitro drug release studies showed that the prepared microspheres exhibited prolonged drug release upto 62.89% for more than 9 h. The mechanism of drug release was found to be a combination of both peppas and matrix kinetics. Thus the developed floating microspheres of cinnarizine may be used as sustained drug delivery system for increasing the therapeutic efficacy with an improved patient compliance.

scholarly journals Development and Characterization of Mitoxantrone-Loaded Glutaraldehyde Crosslinked Sodium Alginate Nanoparticles for the Delivery of Anticancer Drugs

2021 ◽  
pp. 18-24
Author(s):  
Muhammad Wahab Amjad ◽  
Maria Abdul Ghafoor Raja
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sodium Alginate ◽  
Anticancer Drugs ◽  
Antineoplastic Agent ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency

Every year millions of new cases of various types of cancers are diagnosed, leading to an alarming rate of fatalities. Mitoxantrone is an anthracenedione antineoplastic agent which is used in the treatment of various types of cancer, mostly acute myeloid leukemia and prostate cancer. In spite of its therapeutic applications, it possesses numerous limitations and side effects including specific targeting and systemic toxicity. Sodium alginate is a biodegradable, mucoadhesive and biocompatible polymer commonly used in drug delivery applications. Glutaraldehyde is a saturated dialdehyde and is used as a polymer cross linker. In this study, mitoxantrone-loaded glutaraldehyde-sodium alginate nanoparticles were developed by ionic gelation method and characterized (determination of particle size, drug entrapment efficiency, drug release and its kinetics) for the delivery of anticancer drugs. The nanoparticles mean particle size was found to be within the acceptable range. The entrapment efficiency was also on the higher side with sustained drug release. The findings of this study reveal promising potential of delivery system and project the way forward for further in vitro and in vivo investigations.

scholarly journals FORMULATION AND IN VITRO IN VIVO EVALUATION OF BOSENTAN PELLETS FOR PROLONGED DRUG RELEASE

2018 ◽  
Vol 11 (8) ◽  
pp. 498
Author(s):  
Narender Karra ◽  
Narayana Raju P ◽  
Sivakumar R
Keyword(s):  
Drug Release ◽  
Half Life ◽  
Elimination Rate ◽  
Pulmonary Artery Hypertension ◽  
Maximum Plasma ◽  
In Vivo Evaluation ◽  
Pore Former ◽  
Fluid Bed

Objective: The objective of this study was to develop extended release (ER) pellets of Bosentan, an endothelin receptor antagonist using fluid bed processor (coating).Method: The ER drug pellets of Bosentan were prepared using fluid bed coating. These drug-loaded pellets were further coated with ethyl cellulose of two viscosity grades and Eudragit as rate controlling polymers individual and in combination, hypromellose as pore former and binder, acetyl tributyl citrate as plasticizer, and magnesium stearate as anti-adhering agent.Results: The drug release was extended up to 24 h, and the drug release was mainly depends on the polymer type and polymer proportion. In vivo study of Bosentan, ER pellets were performed in healthy rabbits (New Zealand, White) of either sex weighing (3.0–3.3 kg) and were divided into two separate groups, each group consisting of 6 animals. Maximum plasma concentration (Cmax), maximum time (Tmax), area under the curve (AUC0-t), elimination rate constant (Kel), and half-life (T1/2) were studied for optimized formulation. Formulation was releasing the drug for a prolonged period of time.Conclusion: By the above results, it was observed that the prepared pellets could release the drug for an extended period when compared with the conventional dosage form of Bosentan, optimized formulation was shown longer half-life and Cmax indicates its acceptability. Finally, ER pellets of Bosentan were prepared for the treatment of pulmonary artery hypertension by fluid bed processor.

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 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.  

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