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

Author(s):  
SUDIPTA DAS ◽  
RIMI DEY

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.

2018 ◽  
Vol 10 (2) ◽  
pp. 52 ◽  
Author(s):  
Akshay Singha Roy ◽  
Sudipta Das ◽  
Arnab Samanta

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).


Author(s):  
Niyati Shah ◽  
Ayesha Sheikh ◽  
Hitesh Jain

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.


2017 ◽  
Vol 9 (6) ◽  
pp. 21 ◽  
Author(s):  
Rajalakshmi S. V. ◽  
Vinaya O. G.

Objective: Aim of the study was to formulate, evaluate and optimize medicated Lip rouge containing acyclovir encapsulated inside a novel vesicular carrier, niosome so that the formulation can improve its membrane penetration. Formulating as a cosmetic Lip rouge formulation will also improve patient compliance in the treatment of herpes labialis.Methods: Acyclovir niosomes were prepared by thin film hydration method. Niosomes were evaluated and were optimized by considering the entrapment efficiency and in vitro release profile. The optimized niosomes were incorporated into lipstick, lip balm and lip rouge for selecting the best lip formulation. Based on the in vitro release profile, ease of application and properties of prepared formulations lip rouge was selected and further evaluations were carried out.Results: Among the six formulations of niosomes NF2 has showed 88.49 % entrapment efficiency and 86.97% cumulative drug release in 8 h. The formulation was optimized considering both entrapment efficiency and in vitro release. The optimized formulation of niosomes was incorporated into Lipstick, lip balm and lip rouge. The evaluation results of lipstick, lip balm and lip rouge for in vitro release suggested lip rouge as the best formulation. The percentage cumulative release of drug from optimized lip rouge at the end of 8 h was 84.77%. The percentage cumulative drug release in ex vivo studies for 8 h was 60.88 %.Conclusion: The results suggested that prepared lip rouge containing acyclovir niosomes can effectively deliver the drug than the marketed acyclovir cream and successful therapy of Recurrent Herpes labialis can be achieved.


2008 ◽  
Vol 25 (6) ◽  
pp. 1387-1395 ◽  
Author(s):  
Elizabeth R. Proos ◽  
James H. Prescott ◽  
Mark A. Staples

Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.


Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai

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.


Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S

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.


Author(s):  
V K Verma ◽  
Ram A

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 


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