scholarly journals Study of the Effect of Dillenia indica Fruit Mucilage on the Properties of Metformin Hydrochloride Loaded Spray Dried Microspheres

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Hemanta Kumar Sharma ◽  
Lila Kanta Nath

Natural materials are preferred over synthetic counterparts because of their biodegradable and biocompatible nature. The present work was proposed to utilize mucilage from natural source for the development of controlled release formulation of metformin hydrochloride. Natural mucilaginous substance extracted from Dillenia indica L. (DI) fruit was used in fabricating controlled release microspheres. The microspheres were prepared by spray drying method under different formulation parameters. The prepared microspheres were studied for particle size, drug excipient compatibility, particle shape and surface morphologies, drug entrapment efficiency, mucoadhesivity, and in vitro drug release properties. The prepared microspheres exhibited mucoadhesive properties and demonstrated controlled release of metformin hydrochloride. The study reveals that the natural materials can be used for formulation of controlled release microspheres and would provide ample opportunities for further study.

2013 ◽  
Vol 63 (2) ◽  
pp. 209-222 ◽  
Author(s):  
Hemanta Kumar Sharma ◽  
Sunita Lahkar ◽  
Lila Kanta Nath

The present work envisages utilisation of biodegradable and biocompatible material from natural sources for the development of controlled release microspheres of metformin hydrochloride (MetH). Natural polysaccharides extracted from Dillenia indica L. (DI), Abelmoschus esculentus L. (AE) and Bora rice flour were used in fabricating controlled release microspheres. The microspheres were prepared by the emulsion solvent diffusion technique with different proportions of natural materials and were studied for entrapment efficiency, particle size, particle shape, surface morphology, drug excipient compatibility, mucoadhesivity and in vitro release properties. The prepared microspheres showed mucoadhesive properties and controlled release of metformin hydrochloride. The study has revealed that natural materials can be used for formulation of controlled release microspheres and will provide ample opportunities for further study


2018 ◽  
Vol 8 (5-s) ◽  
pp. 378-387
Author(s):  
Mrs Kalpna ◽  
Druv Dev ◽  
Mohammad Shahnaz ◽  
Jyoti Parkash ◽  
DN Prasad

In this work an attempt was made for the preparation and evaluation of controlled release chitosan microspheres using anti-diabetes drug Metformin hydrochloride. The microspheres were prepared by Ionotropic gelation method using chitosan as polymer and Sodium Tripolyphosphate (TPP) as crosslinking agent. The compatibility of drug and polymer is analyzed by using FTIR and DSC method. There was no interaction detected by FTIR and DSC study. Further the prepared microspheres were evaluated for particle size, drug entrapment efficiency, surface morphology, drug content, drug loading and in vitro drug release. Amongst all the formulation batch 7 shows the best release when compared to other batch. SEM (Scanning electron microscopy) revealed that microspheres were spherical and porous. Finally it was concluded that Metformin hydrochloride loaded chitosan – TPP microspheres have been found suitable for controlled release formulation due to its bioavailability and biodegradability and thus lead to improved patient compliance. Keywords: Microspheres, Metformin hydrochloride, Ionotropic gelation method, chitosan.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 765
Author(s):  
Nouran O. Abdelmageed ◽  
Nadia M. Morsi ◽  
Rehab N. Shamma

The application of intra-articular injections in osteoarthritis management has gained great attention lately. In this work, novel intra-articular injectable hyaluronic acid gel-core vesicles (hyaluosomes) loaded with diacerein (DCN), a structural modifying osteoarthritis drug, were developed. A full factorial design was employed to study the effect of different formulation parameters on the drug entrapment efficiency, particle size, and zeta potential. Results showed that the prepared optimized DCN- loaded hyaluosomes were able to achieve high entrapment (90.7%) with a small size (310 nm). The morphology of the optimized hyaluosomes was further examined using TEM, and revealed spherical shaped vesicles with hyaluronic acid in the core. Furthermore, the ability of the prepared DCN-loaded hyaluosomes to improve the in vivo inflammatory condition, and deterioration of cartilage in rats (injected with antigen to induce arthritis) following intra-articular injection was assessed, and revealed superior function on preventing cartilage damage, and inflammation. The inflammatory activity assessed by measuring the rat’s plasma TNF-α and IL-1b levels, revealed significant elevation in the untreated group as compared to the treated groups. The obtained results show that the prepared DCN-loaded hyaluosomes would represent a step forward in the design of novel intra articular injection for management of osteoarthritis.


Author(s):  
Chetankumar Mutagond ◽  
Vinod M R ◽  
Vijapure V M ◽  
Marapur S C ◽  
R G Patil ◽  
...  

The present study sought to develop and evaluate spray-dried microspheres of chitosan and xanthan gum for controlled release of ramipril, a widely used antihypertensive drug. The prepared microspheres were characterized by particle size analysis, scanning electron microscopic studies, differential scanning calorimetric analysis, Fourier transform infrared spectroscopy analysis, X-ray diffraction studies, drug entrapment efficiency, and in-vitro drug release study. The prepared microspheres were spherical in shape and freely flowing. The size of the microspheres was in the range of 25.7 to 47.4 µm and the drug entrapment efficiency was in the range of 74.68% to 90.44%. TheDSC analysis and X-ray diffraction studies indicated that the drug was uniformly dispersed in amorphous state in the microspheres. The in-vitro drug release indicated that the spray-dried microspheres prepared with chitosan alone were not suitable for controlled released delivery of drug as maximum amount of drug was released within 5 hrs. Whereas microspheres prepared by xanthan gum released small amount of drug within 5 hrs and more amount of drug was controlled released that fit the therapeutic needs. Drug release mechanism followed non-Fickian transport. These suggest the formulation potential of chitosan and xanthan gum for spray-dried microspheres for controlled release of ramipril


Author(s):  
Yasir Mohd ◽  
A Bhattacharyya ◽  
M Bajpai ◽  
M Yasir ◽  
M Asif

A floating type dosage form, gel beads of metformin hydrochloride was prepared by emulsification gelation technique. The gel bead was formed by mixing the polymer in water, oil phase and it was extruded in the calcium chloride solution as curing agent. The formulation parameters optimized were polymer ratio, concentration of oil, curing time on drug content, floating lag time, morphology, swelling of beads and release kinetics.The scanning electron photomicrographs revealed morphology of beads. The size of beads was measured. Entrapment efficiency of drug loaded beads was found to be over 90%. In vitro release of metformin hydrochloride from alginate–pectin beads into simulated gastric fluid at 37 ºC showed no significant burst effect. The cumulative release reached above 74.71 ± 4.15% in about 12h. The use of sodium alginate and combinations of sodium alginate with pectin were used to study the effect on the sustained release of the drug from the formed beads. It was found that sodium alginate was not sufficient to sustain the drug release at gastric pH (fed condition). Appropriate combination of alginate and pectin could provide the sustained release of drug. Floating gel beads formulation provides an alternative delivery for metformin in diabetes treatment.


Author(s):  
Priyangi Roy ◽  
Purusattam Gartia ◽  
Aritra Nayek ◽  
Asok Kumar Samanta

The aim of the study was to prepare gefitinib-loaded polycaprolactone microcapsules by simple conventional solvent evaporation method with a view to achieve controlled release of the drug following subcutaneous administration once in a week for targeted therapeutic action especially locally. The microcapsules were prepared using different drug-polymer ratios (1:2, 1:4 and 1:6) and three different stabilizers/surfactants (0.25% w/v, 0.50% w/v and 0.75% w/v) concentrations in aqueous phase. Depending upon the formulation variables, the highest drug entrapment efficiency and the lowest average particle size diameter of the microcapsules were found to be respectively 90.19±2.61 % and 201±3.05 µ. Comparison of Fourier Transform Infra Red spectra of gefitinib, polycaprolactone, their physical mixture and the drug- loaded microcapsules showed the absence of drug -polymer interaction .The in-vitro dissolution study showed that the release of drug from the microcapsules was almost complete on day seventh and the drug release followed Higuchi model.


Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


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.


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