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Fulltext Solid-state characterization studies and effect of PEG 20000 and P90G on particle size reduction and stability of complexed glimepiride nanocrystals

Sajeev Kumar B, Saraswathi R, Dhanaraj SA

J Young Pharm, 2013 Sep;5(3):83-9.
PMID: 24396247 DOI: 10.1016/j.jyp.2013.08.002

OBJECTIVE: The objective of the present study is to formulate and characterize the properties of complexed glimepiride nanocrystals (GLP) by various techniques at different stages of its development, and to study the effect of PEG 20000 and P90G on particle size reduction and stability of nanocrystals.
METHOD: Precipitated (GLP-PEG) and complexed NCs (GLP-PEG-P90G) of glimepiride were characterized for particle size, size distribution, zeta potential and stability assessment using photon correlation spectroscopy (PCS). The crystallinity was analyzed using differential scanning calorimetry (DSC) and X-ray powder diffraction spectroscopy (XRPD). The surface morphology and chemical stability were assessed by means of scanning electron microscopy (SEM) and infrared spectroscopy (FTIR).
RESULTS: A formulation with drug-polymer ratio of 1:1 was most ideal in developing stable NCs as it exhibited smaller particle size and high stability. A high zeta potential was observed in all NCs after complexation indicating improved stability. DSC and XRPD studies showed no change in crystallinity after complexation. SEM analysis of complexed NCs showed presence of spherical shape particles (size below 1 μm) with a lipid coat on the surface. Stability studies on optimized formulation (F1) revealed no change in particle size during 3-month period. FTIR studies prove that the chemical identity of GLP was preserved in the samples and the formulation was stable.
CONCLUSION: Solid-state characterization studies reveal that complexed GLP NCs are promising carriers for drug delivery and they can be safely and effectively used in design of various formulations. Also, PEG 20000 and P90G are excellent polymer and lipid for particle size reduction (nanonization) and stabilization of nanocrystals.
Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery

Kumar BS, Saraswathi R, Kumar KV, Jha SK, Venkates DP, Dhanaraj SA

Drug Deliv, 2014 May;21(3):173-84.
PMID: 24102185 DOI: 10.3109/10717544.2013.840690

Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (<1000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.

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