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 Formulation and Evaluation of sustained release Microspheres of Atorvastatin using Chitosan and Alginate

2017 ◽  
Vol 9 (3) ◽  
Author(s):  
Y. M. Charde ◽  
S. G. Dhage ◽  
G. K. Lohiya ◽  
J. G. Avari
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Binding ◽  
Encapsulation Efficiency ◽  
Low Cost ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation

Certain problems regarding the drugs like high first pass metabolism, also the bioavailability of the certain drugs varies due to instability in acidic environment of stomach. Hence, to resolve such problems the drug should be incorporated in the microspheres for sustained release using a suitable polymer. Natural polymer like chitosan gained great interest in pharmaceutical sector because of its advantages like biodegradability, biocompatibility, non-toxicity, non-immunogenicity and low cost. In the present study, formulation and evaluation of polymeric microspheres of Atorvastatin Calcium was carried out and the release profile of such drug using the alginate and chitosan was studied. Microspheres were prepared for sustained release of drug using chitosan and alginate polymers by ionotropic gelation method. Microspheres were spherical in shape, having good flow properties and further its encapsulation efficiency, swelling index, micromeritic study, in- vitro drug release study and stability studies were performed in order to characterize microspheres. Three different concentrations of sodium alginate (1%, 2% and 3%) were used. The higher encapsulation efficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in the polymeric chains and consequently the greater degree of cross linking. The highest encapsulation efficiency (88.36) was achieved with 2% w/v sodium alginate in combination with 3% chitosan (F6). Among the prepared formulations with respect to the entrapment efficiency, swelling studies and in vitro drug release, the alginate-chitosan microspheres prepared by ionotropic gelation using calcium chloride found to be better than ionically cross linked alginate spheres alone. Therefore, dual cross-linked, microspheres are promising carrier for sustained release of drug.

scholarly journals FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Loading ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Polyvinyl Pyrrolidone ◽  
Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

scholarly journals Development of Oral Sustained Release Rifampicin Loaded Chitosan Nanoparticles by Design of Experiment

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Bhavin K. Patel ◽  
Rajesh H. Parikh ◽  
Pooja S. Aboti
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Sustained Release ◽  
Design Of Experiment ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Release Kinetic

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X1), concentration of tripolyphosphate (X2), and homogenization speed (X3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.

scholarly journals Formulation and evaluation of lansoprazole loaded enteric coated microspheres

2020 ◽  
Vol 1 (4) ◽  
pp. 124-130
Author(s):  
SK. Haneesha ◽  
M. Venkataramana ◽  
N. Ramarao
Keyword(s):  
Drug Release ◽  
Intestinal Absorption ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Film Coating ◽  
In Vitro Drug Release ◽  
Evaporation Technique ◽  
Drug Entrapment Efficiency ◽  
Enteric Coated

The research focuses on the development of multiparticulate delivery system for acid-labile Lansoprazole to prevent its degradation in the acidic environment of the stomach and enhance its bioavailability via intestinal absorption. This problem can be solved by enteric coating. In this project, cellulose acetate phthalate a polymer usually utilized for gastrointestinal film coating of tablets, was used to prepare enteric microspheres of lansoprazole with solvent evaporation technique in various formulations such as F1, F2, F3, F4, F5 with drug: polymer ratios of 1:1, 1:2, 1:3, 1:4, 1:5 respectively. FTIR study indicated compatibility between drug and polymer. Increase in concentration of polymer increased spheriocity and mean diameter of the microspheres. The drug entrapment efficiency was in the range of 72.23% to 88.64%. SEM revealed that microspheres were found spherical and porous. In-vitro study proves that drug release slowly increases as the pH of the medium increased and prevents degradation of drug in acidic pH. In-vitro drug release was found to be 92.80%, 94.55%, 92.72%, 96.34%, 98.65% in all 5 formulations. All 5 formulations showed gastric resistance around 80-90%. So it is concluded that the developed enteric coated microspheres of Lansoprazole prevented drug release in the stomach which would lead to significant improvement in its bioavailability through enhanced intestinal absorption.

scholarly journals Formulation Development and Optimization of Sustained Release Microspheres of Acebrophylline

2021 ◽  
pp. 13-28
Author(s):  
Niyati Shah ◽  
Ayesha Sheikh ◽  
Hitesh Jain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Kinetic ◽  
Vitro Release ◽  
Polymer Ratio ◽  
Sustained Release Microspheres

Objectives: Aim of present work is to prepare and evaluate Sustained release microspheres of Acebrophylline for treatment of Asthma. Experimental work: In present investigation, attempt was made to prepare sustained release microspheres of Acebrophylline with different polymer ratio using Ionic gelation method. Drug- excipient compatibility studies were performed by FTIR. The best suited Microspheres formulation was found on the basis production yield, entrapment efficiency and in vitro release study. Optimized batch of microspheres (B2) was characterized for FTIR, DSC, and SEM analysis. The drug release data of optimized batch was fitted into different release kinetic models. The optimized batch of microspheres (B2) was subjected for the short term stability study at 40 ± 2°C with RH of 75% for a period of 1 month. Results and discussion: There was no interaction found between drug and excipients. Sodium alginate (2%) concentration, Eudragit RS-100 (1:2) ratio gave highest sustainable property and CaCl2 (2.5%) concentration had a good cross linking property. This observation done on the basis of production yield, entrapment efficiency and In vitro release study. The Microspheres prepared from Ionic gelation method had Drug : Eudragit RS100 (1:2), 2 % Sodium alginate and 2.5 % CaCl2 (B2) give 99.2 % drug release over the periods of 12 hr. The drug release from optimized microspheres formulation (B2) follows first order release kinetic. DSC study showed the melting behavior of drug present into microspheres. SEM studies showed that optimized microspheres were spherical and rough surface.  Stability study proved that optimized formulation (B2) was stable. Conclusion:  Drug: Polymer ratio and Volume of CaCl2 had significant effect on % Entrapment efficiency and Drug release. From the Scanning Electron Microscopy (SEM) study observed that microspheres was spherical and rough surface. Non Fickian diffusion was the mode of drug release from Acebrophylline- loaded microspheres. After stability study no physical changes & almost same drug release was observed in microspheres. Hence, the formulation B2 was stable.

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 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.

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.

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