Formulation and evaluation of Nimodipine-loaded solid lipid nanoparticles delivered via lymphatic transport system

Chalikwar, Shailesh S.; Belgamwar, Veena S.; Talele, Vivek R.; Surana, Sanjay J.; Patil, Mrunal U.

doi:10.1016/j.colsurfb.2012.04.027

Cited by 126 publications

(61 citation statements)

References 35 publications

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“…In the recent decades, nanospheres [8-12, 15, 16, 18] or microspheres [11,13,14,17] were widely used as drug carriers. A few reports have been published on the use of liquid and solid microemulsions [19,20], solid dispersions [21][22][23] or drug-loaded type systems based on cyclodextrins [24][25][26] and lipid [27][28][29] or phospholipid micelles [30,31]. Nevertheless, all these systems have organic character, so are potentially sensitive to external factors such as temperature or pH, and can drastically change their properties under the effect of these factors [32].…”

Section: Introductionmentioning

confidence: 99%

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

et al. 2015

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Two mesoporous silica materials: MCM-41 and SBA-15 were applied as potential nanocarriers for poorly soluble drug-nimodipine. Drug incorporation was performed using modified adsorption from the solution method and loaded samples before and after washing procedure were studied. The physical properties were verified by: differential scanning calorimetry, X-ray powder diffraction, electron microscopies (SEM/TEM) and Fourier-transform infrared spectroscopy (FT-IR). FT-IR results for bulk nimodipine were interpreted on the basis of first principles calculations (DFT). As a result of encapsulation process, in both matrices nimodipine appeared simultaneously in two forms: crystalline and amorphous, but the first one turned out to be easily removable during washing procedure. The in vitro dissolution and release tests were performed with ultra pure water under supersaturating conditions. The release rate of the amorphous nimodipine from mesoporous silica materials was at least 70 times higher than dissolution rate of bulk drug, thus revealed a potential usefulness of such carrier in future pharmaceutical applications in terms of delivery of poorly soluble drugs.

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Section: Introductionmentioning

confidence: 99%

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

et al. 2015

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“…Such enhancement could be explained by the following aspects: (1) the potent ability of Cur in inhibiting P-gp efflux pump and the increased mucosal adhesion and intestinal permeability by CMCS; (2) the high stability of CNC/LHR MPMs upon dilution in physiological fluid, along with the increased stability and water solubility of Cur and CsA; (3) the small particle size of CsA-CNC/ LHR MPMs that can be absorbed in their intact form away from P-gp recognition through an endocytic pathway. Additionally, the lymphatic transport of CNC/LHR MPMs through M cells might further increase the drug absorption (Chalikwar et al, 2012;Indu et al, 2013;Patil-Gadhe et al, 2014); (4) the ability of CNC/LHR MPMs to evade the rapid uptake by the reticuloendothelial system (RES), resulting in prolonged circulation time. To sum up, the encapsulated CsA in MPMs might be absorbed as intact micelles away from P-gp recognition, as a P-gp-independent way.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

Curcumin-carboxymethyl chitosan (CNC) conjugate and CNC/LHR mixed polymeric micelles as new approaches to improve the oral absorption of P-gp substrate drugs

et al. 2016

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The low oral bioavailability of numerous drugs has been mostly attributed to the significant effect of P-gp-mediated efflux on intestinal drug transport. Herein, we developed mixed polymeric micelles (MPMs) comprised of curcumin-carboxymethyl chitosan (CNC) conjugate, as a potential inhibitor of P-gp-mediated efflux and gastrointestinal absorption enhancer, and low-molecular-weight heparin-all-trans-retinoid acid (LHR) conjugate, as loading material, with the aim to improve the oral absorption of P-gp substrate drugs. CNC conjugate was synthesized by chemical bonding of curcumin (Cur) and carboxymethyl chitosan (CMCS) taking advantage of the inhibition of intestinal P-gp-mediated secretion by Cur and the intestinal absorption enhancement by CMCS. The chemical structure of CNC conjugate was characterized by 1 H NMR with a degree of substitution of Cur of 4.52-10.20%. More importantly, CNC conjugate markedly improved the stability of Cur in physiological pH. Cyclosporine A-loaded CNC/LHR MPMs (CsA-CNC/LHR MPMs) were prepared by dialysis method, with high drug loading 25.45% and nanoscaled particle size ($200 nm). In situ single-pass perfusion studies in rats showed that both CsA + CNC mixture and CsA-CNC/LHR MPMs achieved significantly higher K a and P eff than CsA suspension in the duodenum and jejunum segments (p5 0.01), which was comparable to verapamil coperfusion effect. Similarly, CsA + CNC mixture and CsA-CNC/LHR MPMs significantly increased the oral bioavailability of CsA as compared to CsA suspension. These results suggest that CNC conjugate might be considered as a promising gastrointestinal absorption enhancer, while CNC/LHR MPMs had the potential to improve the oral absorption of P-gp substrate drugs.

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“…In addition, the process can be modulated for obtaining desired drug release and the entrapped drug can be protected against chemical/enzymatic degradation. Hence, SLNs are considered to be better alternative than polymeric nanoparticles, liposomes, microemulsions, nanoemulsions and self-emulsifying drug delivery systems [2][3][4][5][6][7][8][9][10].…”

Section: Optimization By Factorial Designmentioning

confidence: 99%

Formulation Optimization of Rosuvastatin Calcium-Loaded Solid Lipid Nanoparticles by 32 Full-Factorial Design

Dhoranwala¹,

Shah²,

Shah³

2016

NanoWorld J

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Formulation and evaluation of Nimodipine-loaded solid lipid nanoparticles delivered via lymphatic transport system

Cited by 126 publications

References 35 publications

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

Curcumin-carboxymethyl chitosan (CNC) conjugate and CNC/LHR mixed polymeric micelles as new approaches to improve the oral absorption of P-gp substrate drugs

Formulation Optimization of Rosuvastatin Calcium-Loaded Solid Lipid Nanoparticles by 32 Full-Factorial Design

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