A novel surface modified nitrendipine nanocrystals with enhancement of bioavailability and stability

Quan, Peng; Shi, Kai; Piao, Hongze; Piao, Hongyu; Liang, Na; Xia, Dengning; Cui, Fude

doi:10.1016/j.ijpharm.2012.04.025

Cited by 51 publications

(17 citation statements)

References 24 publications

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“…This plateau in ZP values suggested a complete saturation of CS-DNS surface with the adsorbed positively charged CS. 43 CS-DNS-F10 was selected as our nominated coated formula along with uncoated DNS-F7 for further studies.…”

Section: Cs-dnsmentioning

confidence: 99%

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Allam¹,

Hamdallah²,

Abdallah³

2017

IJN

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Nanodrug delivery systems have been widely reviewed for their use in several drug formulations to improve bioavailability, sustain effect, and decrease side effects of many candidate drugs. The objective of this study was to evaluate the potential of chitosan (CS)-coated nanosuspensions to enhance bioavailability and reduce the diarrheal side effect of diacerein (DCN) after oral administration. DCN nanosuspensions (DNS) were prepared by sonoprecipitation technique using different stabilizers at three different concentrations. The selected DNS with optimum particle size (PS), polydispersity index (PDI), and Zeta potential (ZP) was coated with three different concentrations of CS-coated DNS (CS-DNS) and screened. In vitro dissolution was performed for the selected lyophilized formulae and compared with DCN powder in addition to the assessment of drug crystallinity via scanning electron microscopy, X-ray powder diffraction, and differential scanning calorimetry. Ex vivo drug permeability using noneverted rat intestine, intraluminal content, and mucoadhesion evaluation was studied for nominated formulae in comparison to DCN suspension. Moreover, in vivo study, pharmacokinetic parameters, and evaluation of diarrheal potential were conducted after oral administration of selected formulae. Polyvinyl pyrrolidone (PVP)-stabilized DNS showed a significant increase ( P ≤0.05) in PS and PDI as the stabilizer concentration increased. PVP-stabilized DNS with the lowest CS concentration was protected from aggregation by lyophilization with mannitol. A remarked enhancement in dissolution parameters was observed in the nanocrystals’ formulae. Morphological examination and X-ray diffraction confirmed drug crystallinity. The intermediate permeation parameters of CS-DNS-F10, lowest rhein-to-DCN ratio in intraluminal content along with the highest percentage of mucoadhesive, could serve as a sustaining profile of coated formula. CS-DNS-F10 showed a significantly higher C max of 0.74±0.15 µg/mL at a delayed T max of 3.60±0.55 hours with a relative bioavailability of 172.1% compared to DCN suspension. CS-coated nanosuspensions could serve as promising revenue to enhance bioavailability and reduce the diarrheal side effect of DCN after oral administration.

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Section: Cs-dnsmentioning

confidence: 99%

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Allam¹,

Hamdallah²,

Abdallah³

2017

IJN

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“…Previous reports mentioned similar finding of low zeta potential value for nitrendipine nanosuspensions prepared using PVA. 28 The authors also mentioned improvement in this value and production of constant particle size following surface modification of the particles after incorporation of cationic polymer such as chitosan. Improvement of the obtained zeta potential value will be studied in our upcoming work by optimizing the concentration of different cationic and anionic polymer.…”

mentioning

confidence: 99%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability.

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“…Cefixime trihydrate has limited solubility in buffer but is soluble in methanol; hence methanol was added to PBS pH 6.8 to maintain the perfect sink conditions 32 . The beakers were placed on magnetic stirrers and stirred with magnetic beads and were covered with paraffin film to prevent any evaporative loss during the experimental run 33 . Aliquots were withdrawn from the receptor compartments at periodic time intervals for 24 hours and replaced with equivalent amounts of fresh diffusion medium.…”

Section: Drug Release Studymentioning

confidence: 99%

Untitled

2018

IJPSR

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ABSTRACT:Cefixime trihydrate belongs to third generation cephalosporin having poor water solubility. In the present study, nanocrystal suspensions of cefixime trihydrate were prepared with the objective of providing enhanced solubility and stability with reduced particle size and thus improving the bioavailability potential. Nanocrystal suspensions were prepared by high pressure homogenization technique and evaluated for particle size, polydispersity index, zeta potential, and drug release. 2 3 factorial design was used for the formulation designing purpose. Particles of average size 143.5nm having PDI of 0.269 were produced. Zeta potential was found to be -36.6mV and the formulation was found stable on the basis of results obtained from differential scanning calorimetry and scanning electron microscopy studies. The drug release and ex-vivo permeation studies revealed enhanced permeation of drug, as desired, indicating its potential for an attempt towards successful nanocrystal formulation.

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A novel surface modified nitrendipine nanocrystals with enhancement of bioavailability and stability

Cited by 51 publications

References 24 publications

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Chitosan-coated diacerein nanosuspensions as a platform for enhancing bioavailability and lowering side effects: preparation, characterization, and ex vivo/in vivo evaluation

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

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