Chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol

Abstract

Background and the purpose of the studyCarvedilol nonselective β-adrenoreceptor blocker, chemically (±)-1-(Carbazol-4-yloxy)-3-[[2-(o-methoxypHenoxy) ethyl] amino]-2-propanol, slightly soluble in ethyl ether; and practically insoluble in water, gastric fluid (simulated, TS, pH 1.1), and intestinal fluid (simulated, TS without pancreatin, pH 7.5) Compounds with aqueous solubility less than 1% W/V often represents dissolution rate limited absorption. There is need to enhance the dissolution rate of carvedilol. The objective of our present investigation was to compare chitosan and chitosan chlorhydrate based various approaches for enhancement of dissolution rate of carvedilol.MethodsThe different formulations were prepared by different methods like solvent change approach to prepare hydrosols, solvent evaporation technique to form solid dispersions and cogrind mixtures. The prepared formulations were characterized in terms of saturation solubility, drug content, infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), electron microscopy, in vitro dissolution studies and stability studies.ResultsThe practical yield in case of hydrosols was ranged from 59.76 to 92.32%. The drug content was found to uniform among the different batches of hydrosols, cogrind mixture and solid dispersions ranged from 98.24 to 99.89%. There was significant improvement in dissolution rate of carvedilol with chitosan chlorhdyrate as compare to chitosan and explanation to this behavior was found in the differences in the wetting, solubilities and swelling capacity of the chitosan and chitosan salts, chitosan chlorhydrate rapidly wet and dissolve upon its incorporation into the dissolution medium, whereas the chitosan base, less water soluble, would take more time to dissolve.ConclusionThis technique is scalable and valuable in manufacturing process in future for enhancement of dissolution of poorly water soluble drugs.

Electrospun Biomaterials in the Treatment and Prevention of Scars in Skin Wound Healing

“…However, it is important to note that with polymers like chitosan there are drawbacks. Chitosan, as an example, is poorly soluble (Shete et al, 2012), and so tends to be dissolved in acidic conditions, namely using acetic acid or trifluoroacetic acid for example (Geng et al, 2005;Bazmandeh et al, 2019;Gu et al, 2019). The toxicity and cost associated with such solvents can imped the potential of chitosan in wound and anti-scarring therapies (Mengistu Lemma et al, 2016), however, during the electrospinning process much of the solvent evaporates under ideal conditions, and so could help alleviate these unwanted side effects when harsher solvents are required (Golecki et al, 2014;Haider et al, 2015).…”

Fabrication of Niclosamide loaded solid lipid nanoparticles:in vitrocharacterization and comparativein vivoevaluation

“…Powder X-ray diffraction (JEOL, Tokyo, Japan) technique was applied to analyse crystalline nature of NCS (drug) and NFM-3 [24]. P-XRD analysis was carried out by CuKa radiation and scanned up to 80 , step size 2Ø-0.05 and step time 1.0 s, divergence slit 1 , receiving slit 0.2 mm and scattering slit 1 .…”

Development of carvedilol-cyclodextrin inclusion complexes using fluid-bed granulation: a novel solid-state complexation alternative with technological advantages

“…Different strategies have been studied to improve the aqueous solubility of CARV . Inclusion complexation with cyclodextrins using different techniques has been evaluated, resulting in significant improvements in the solubility and dissolution profile of the drug .…”

“…[6] Different strategies have been studied to improve the aqueous solubility of CARV. [7][8][9][10][11][12][13] Inclusion complexation with cyclodextrins using different techniques has been evaluated, resulting in significant improvements in the solubility and dissolution profile of the drug. [14][15][16][17][18][19] Superior enhancement of the dissolution rate was observed when CARV was complexed with hydroxypropyl-b-cyclodextrin (HPbCD).…”