Development of an oral rutin nanocrystal formulation

Mauludin, Rachmat; Müller, Rainer H.; Keck, Cornelia M.

doi:10.1016/j.ijpharm.2008.11.029

Cited by 231 publications

(108 citation statements)

References 33 publications

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“…31 The extent of such changes depends on the chemical and on the physical hardness of the active ingredient, as well as on the applied power density. 32 Therefore, before and following particle-size reduction, DSC and XRD analyses were conducted to assess if the initial crystalline state was preserved. Figure 7 shows the XRD pattern of BCN-SNS.…”

mentioning

confidence: 99%

Process optimization and evaluation of novel baicalin solid nanocrystals

Yue¹,

Liu²,

Wan³

et al. 2013

IJN

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confidence: 99%

Process optimization and evaluation of novel baicalin solid nanocrystals

Yue¹,

Liu²,

Wan³

et al. 2013

IJN

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“…46 The selected lyophilized formulas (F8 and F12) were tested for their PS and PDI, after reconstitution, in the absence and presence of cryoprotectant (mannitol or sucrose). This was done to select the most suitable cryoprotectant that could prevent the aggregation of nanoparticles after lyophilization.…”

Section: Lyophilization Of Prepared Nanosuspensionsmentioning

confidence: 99%

Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers

Elsayed¹,

Abdelbary²,

Elshafeey³

2014

IJN

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Context Diacerein (DCN) has low aqueous solubility (3.197 mg/L) and, consequently, low oral bioavailability (35%–56%). To increase both the solubility and dissolution rate of DCN while maintaining its crystalline nature, high pressure homogenization was used but with only a few homogenization cycles preceded by a simple bottom-up technique. Methods The nanosuspensions of DCN were prepared using a combined bottom-up/top-down technique. Different surfactants – polyvinyl alcohol, sodium deoxycholate, and sodium dodecyl sulfate – with different concentrations were used for the stabilization of the nanosuspensions. Full factorial experimental design was employed to investigate the influence of formulation variables on nanosuspension characteristics using Design-Expert ® Software. Particle size (PS), zeta potential, saturation solubility, in vitro dissolution, and drug crystallinity were studied. Moreover, the in vivo performance of the optimized formula was assessed by bioavailability determination in healthy human volunteers. Results The concentration of surfactant had a significant effect on both the PS and polydispersity index values. The 1% surfactant concentration showed the lowest PS and polydispersity index values compared with other concentrations. Both type and concentration of surfactant had significant effects on the zeta potential. Formula F8 (containing 1% sodium deoxycholate) and Formula F12 (containing 1% sodium dodecyl sulfate) had the highest desirability values (0.952 and 0.927, respectively). Hence, they were selected for further characterization. The saturated solubility and mean dissolution time, in the case of F8 and F12, were significantly higher than the coarse drug powder. Techniques utilized in the nanocrystals’ preparation had no effect on DCN crystalline state. The selected formula (F12) showed a higher bioavailability compared to the reference market product with relative bioavailability of 131.4%. Conclusion The saturation solubility, in vitro dissolution rate and relative bioavailability of DCN were significantly increased after nanocrystallization. Less time and power consumption were applied by the combination of bottom-up and top-down techniques.

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Section: Experimental Questionsmentioning

confidence: 99%

“…The diagnosisbased selection of medicines facilitates providing care from a public health perspective to a large number of patients. Bulk herb extracts of Ruta graveolens, for instance, exert anti-cancer effects [173,174]; and an oral nanoscale formulation of one of its main constituents, rutin, has good bioavailability [175].The nanoparticle form of calcium phosphate has antiproliferative and pro-apoptotic effects on glioma [176] and osteosarcoma [54] cells. Similarly, their homeopathically-manufactured counterparts, e.g., Ruta graveolens 6C and Calcarea Phosphorica 3X [172], are part of a leading combination anti-cancer protocol for gliomas [108,172].…”

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confidence: 99%

Nonlinear Response Amplification Mechanisms for Low Doses of Natural Product Nanomedicines: Dynamical Interactions with the Recipient Complex Adaptive System

Bell

Sarter

Koithan

et al. 2013

J Nanomed Nanotechol

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The purpose of the present paper is (a) to outline the self-organized, complex adaptive network nature of the organism as recipient of nanomedicines; (b) to propose several nonlinear endogenous amplification processes by which pulsed low doses of traditional, homeopathically-manufactured natural product nanomedicines may stimulate a return toward healthier function; and (c) to discuss their potential relevance to novel, but safer than conventional dosing strategies for contemporary nanomedicines. Homeopathy is an over 200-year-old system of complementary and alternative medicine (CAM) that uses low doses of natural plant-, mineral-, and animal-sourced nanomedicines. Homeopathic manufacturing is "green", with mechanical grinding in lactose and agitation in ethanol-water as primary reagents. Agitation within glass containers at room temperature may also contribute nanosilica and nanosilicon as drug delivery vehicles and biological amplifiers. The medicine selection is matched to the recipient organism's systemic patterns of dysfunction and pulsed in the timing of the discrete doses. Endogenous amplification processes within the recipient organism may involve hormesis, time-dependent sensitization, and/or stochastic resonance. Effects are adaptive and systemically diffuse, i.e., causally indirect, rather than pharmacological and local, i.e., direct. All of these nonlinear response processes require interaction of the nanoparticle (NP) dose with the organism as a complex adaptive system. The pulsed NP dose serves as a low intensity salient danger signal for the organism to make network-wide adaptive changes that can lead to healing. The historically safe therapeutic approach of homeopathic nanomedicine dosing avoids risks of high, continuous doses and cumulative toxicity that contemporary nanomedicine researchers are now trying to solve while using NPs as if they were conventional bulk drugs. Integrating the insights, technical procedures, and clinical dosing approaches from modern and homeopathic nanomedicine could lead to major advances in the field for more effective and safer translational applications.NPs in homeopathic medicines [3]. NP concentrations are low, but measurable [3]. Like modern manufactured NPs [13], homeopathicallymanufactured medicines in solution also can exhibit aging effects [9,14]. These nanomedicines are delivered either in ethanolic liquids or sprayed and dried onto lactose or lactose/sucrose pellets for oral administration.Homeopathic manufacturing materials and methods are inherently "green" [15,16]. Previous papers have addressed the striking similarities between modern top-down mechanical attrition procedures for making nanoparticles (NPs) [17] and historical homeopathic medicine manufacturing methods and materials [15,[18][19][20][21]. These similarities include mechanically grinding source materials in lactose for hours and repeatedly agitating ethanol-water solutions containing the source Citation: Bell IR, Sarter B, Koithan M, Standish LJ, Banerji P, et al. (2013) Nonlinea...

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Development of an oral rutin nanocrystal formulation

Cited by 231 publications

References 33 publications

Process optimization and evaluation of novel baicalin solid nanocrystals

Process optimization and evaluation of novel baicalin solid nanocrystals

Nanosizing of a poorly soluble drug: technique optimization, factorial analysis, and pharmacokinetic study in healthy human volunteers

Nonlinear Response Amplification Mechanisms for Low Doses of Natural Product Nanomedicines: Dynamical Interactions with the Recipient Complex Adaptive System

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