Effect of novel stabilizers—cationic polymers on the particle size and physical stability of poorly soluble drug nanocrystals

Sun, Wei; Tian, Wei; Zhang, Yuyang; He, Jianyong; Mao, Shirui; Fang, Liang

doi:10.1016/j.nano.2011.07.006

Cited by 59 publications

(30 citation statements)

References 20 publications

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“…The lyophilized ATR nanocrystals were diluted 80 times with filtered deionized water to obtain ideal concentration range for optimal measurement. 23 (Viscosity values of the dispersion media were made less than equivalent to water [1.0 mPas] at 25°C).…”

Section: Zeta Potential Analysismentioning

confidence: 99%

“…Favorable electrostatic stabilization enhances both in-vitro dissolution and in-vivo efficacy. 23 The anti-hyperlipidemic activity of ATR-CS L nanocrystal formulation was found to be pH dependent. The pharmacodynamic activity of nanocrystal formulation at pH 5 was 2.5-fold higher when compared to pH 6 and marketed product Lipitor ® .…”

mentioning

confidence: 97%

“…22 Identifying an ideal biodegradable stabilizer that can aid in the particle size reduction apart from stabilization of a nanocrystal formulation would be a breakthrough. 23 Chitosan is a deacetylated product of chitin. The cationic charge polymer is biodegradable, biocompatible, nonimmunogenic, 24 and non-toxic which aids its use in oral and intra-venous drug delivery systems.…”

mentioning

confidence: 99%

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Chitosan based atorvastatin nanocrystals: effect of cationic charge on particle size, formulation stability, and in-vivo efficacy

Kurakula¹,

El-Helw²,

Sobahi³

et al. 2015

IJN

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Cationic charged chitosan as stabilizer was evaluated in preparation of nanocrystals using probe sonication method. The influence of cationic charge densities of chitosan (low CS L , medium CS M , high CS H molecular weights) and Labrasol ® in solubility enhancement and modifying the release was investigated, using atorvastatin (ATR) as poorly soluble model drug. Compared to CS M and CS H ; low cationic charge of CS L acted as both electrostatic and steric stabilizer by significant size reduction to 394 nm with charge of 21.5 meV. Solubility of ATR-CS L increased to 60-fold relative to pure ATR and ATR-L. Nanocrystals were characterized for physiochemical properties. Scanning electron microscopy revealed scaffold-like structures with high surface area. X-ray powder diffractometry and differential scanning calorimetry revealed crystalline to slight amorphous state changes after cationic charge size reduction. Fourier transform-infrared spectra indicated no potent drug-excipient interactions. The enhanced dissolution profile of ATR-CS L indicates that sustained release was achieved compared with ATR-L and Lipitor ® . Anti-hyperlipidemic performance was pH dependent where ATR-CS L exhibited 2.5-fold higher efficacy at pH 5 compared to pH 6 and Lipitor ® . Stability studies indicated marked changes in size and charge for ATR-L compared to ATR-CS L exemplifying importance of the stabilizer. Therefore, nanocrystals developed with CS L as a stabilizer is a promising choice to enhance dissolution, stability, and in-vivo efficacy of major Biopharmaceutical Classification System II/IV drugs.

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Section: Zeta Potential Analysismentioning

confidence: 99%

mentioning

confidence: 97%

mentioning

confidence: 99%

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Chitosan based atorvastatin nanocrystals: effect of cationic charge on particle size, formulation stability, and in-vivo efficacy

Kurakula¹,

El-Helw²,

Sobahi³

et al. 2015

IJN

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“…Therefore, stability of the nanometer sized particles is of special importance in order to maintain advantages of nanosuspension and selection of appropriate stabilizers is critical to achieve this goal. As a cationic polymer, chitosan exhibited excellent properties as the stabilizer of itraconazole nanosuspensions, which can provide electrostatic repulsion and steric stabilization effect simultaneously (Sun et al 2012). In addition, size and zeta potential of the nanosuspension particles can be altered by changing chitosan concentration.…”

Section: As Stabilizer Of Nanosuspensions and Emulsionsmentioning

confidence: 99%

“…The release behavior of water soluble drugs can be altered by using chitosan hydrogels, chitosan matrix which can form sustained gel layer (Li et al , 2014Bhattarai et al 2010;Le Tien et al 2003). The dissolution rate and solubility of poorly water soluble drugs can be increased by using chitosan based nano-carriers and chitosan stabilized nanosuspensions (Sun et al 2012;Quan et al 2012). Chitosan based nanocarriers have been widely used as non-viral vectors to overcome the absorption obstacles and increase the transfection efficiency of genes (Mao et al 2010;Buschmann et al 2013).…”

Section: Introductionmentioning

confidence: 99%

Drug Delivery Applications of Chitosan and its Derivatives

Zhang

Mao

2015

Excipient Applications in Formulation Design and Drug Delivery

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The development of drug delivery systems always goes hand in hand with the advancement of material science. The novel synthetic or natural functional materials provide opportunities to design optimal drug delivery systems. Among these, chitosan and its derivatives exhibit excellent application future because of its prominent characteristics. In this chapter, research progress of chitosan and its derivatives for drug delivery, from structure to properties, from properties to its application were overviewed. The physicochemical properties, biological properties, biodegradability, safety evaluation and structure modification of chitosan were introduced. Furthermore, applications of chitosan and its derivatives in drug delivery including as the carrier of nanoparticles and microparticles, as coating material, as matrix of hydrogels, films and sustained release tablets, as stabilizers, as absorption enhancers, were discussed. Finally, the applications of chitosan and its derivatives in different administration routes, and their advantages for gene, protein and vaccine delivery, were reviewed. The numerous successful studies on exploitation and application of chitosan and its derivatives showed promising application future of these materials in drug delivery.

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Excipients and their Functionality for Enabling Technologies in Oral Dosage Forms

Thakkar

Sharma

Khurana

et al. 2016

Pharmaceutical Excipients

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Effect of novel stabilizers—cationic polymers on the particle size and physical stability of poorly soluble drug nanocrystals

Cited by 59 publications

References 20 publications

Chitosan based atorvastatin nanocrystals: effect of cationic charge on particle size, formulation stability, and in-vivo efficacy

Chitosan based atorvastatin nanocrystals: effect of cationic charge on particle size, formulation stability, and in-vivo efficacy

Drug Delivery Applications of Chitosan and its Derivatives

Excipients and their Functionality for Enabling Technologies in Oral Dosage Forms

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