Effect of Crystal Size on the In Vitro Dissolution and Oral Absorption of Nitrendipine in Rats

Xia, Dengning; Cui, Fude; Piao, Hongze; Cun, Dongmei; Piao, Hongyu; Jiang, Yazhen; Ouyang, Mei; Quan, Peng

doi:10.1007/s11095-010-0200-0

Cited by 105 publications

(51 citation statements)

References 40 publications

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“…A previous study found that oral absorption of a drug is influenced by particle size, which affects the dissolution rate. 26 However, the current study found no statistically significant difference in particle size or any other particle characteristics between HMw-NPC and LMw-NPC (Table 1). Thus, particle size and other characteristics might not be responsible for the different bioavailability and absorption results for HMw-NPC and LMw-NPC.…”

contrasting

confidence: 64%

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Tsai¹,

Chang-Liao²,

Chien³

et al. 2012

IJN

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Background: Polylactic-co-glycolic acid (PLGA) nanoparticles have been used to increase the relative oral bioavailability of hydrophobic compounds and polyphenols in recent years, but the effects of the molecular weight of PLGA on bioavailability are still unknown. This study investigated the influence of polymer molecular weight on the relative oral bioavailability of curcumin, and explored the possible mechanism accounting for the outcome. Methods: Curcumin encapsulated in low (5000-15,000) and high (40,000-75,000) molecular weight PLGA (LMw-NPC and HMw-NPC, respectively) were prepared using an emulsificationsolvent evaporation method. Curcumin alone and in the nanoformulations was administered orally to freely mobile rats, and blood samples were collected to evaluate the bioavailability of curcumin, LMw-NPC, and HMw-NPC. An ex vivo experimental gut absorption model was used to investigate the effects of different molecular weights of PLGA formulation on absorption of curcumin. High-performance liquid chromatography with diode array detection was used for quantification of curcumin in biosamples. Results: There were no significant differences in particle properties between LMw-NPC and HMw-NPC, but the relative bioavailability of HMw-NPC was 1.67-fold and 40-fold higher than that of LMw-NPC and conventional curcumin, respectively. In addition, the mean peak concentration (C max ) of conventional curcumin, LMw-NPC, and HMw-NPC was 0.028, 0.042, and 0.057 µg/mL, respectively. The gut absorption study further revealed that the HMw-PLGA formulation markedly increased the absorption rate of curcumin in the duodenum and resulted in excellent bioavailability compared with conventional curcumin and LMw-NPC. Conclusion: Our findings demonstrate that different molecular weights of PLGA have varying bioavailability, contributing to changes in the absorption rate at the duodenum. The results of this study provide the rationale for design of a nanomedicine delivery system to enhance the bioavailability of water-insoluble pharmaceutical compounds and functional foods.

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contrasting

confidence: 64%

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Tsai¹,

Chang-Liao²,

Chien³

et al. 2012

IJN

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“…Moreover, the nanometer-sized particles of carvedilol nanosuspensions could enable the interfacial interaction with the mucin layer, thereby further enhancing the absorption of carvedilol from the intestinal lumen. 21 Meanwhile, SDS used in the nanosuspensions and microsuspensions could improve the intestinal absorption of carvedilol from the intestinal epithelium by the paracellular pathway. 31 The presence of SDS and VES in the suspensions could also contribute to the increased saturation solubility of carvedilol, and thus improve the absorption of the drug.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

“…21,22 However, the preparations used were stabilized by different types or ratios of stabilizers, which may not truly reflect the effects of particle size. Until now, research studies of particle size effect using carvedilol particles stabilized with the same kind and content of stabilizers have scarcely been reported.…”

Section: Introductionmentioning

confidence: 99%

Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation

Liu¹,

Pan²,

He³

et al. 2015

IJN

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The purpose of this work was to explore the particle size reduction effect of carvedilol on dissolution and absorption. Three suspensions containing different sized particles were prepared by antisolvent precipitation method or in combination with an ultrasonication process. The suspensions were characterized for particle size, surface morphology, and crystalline state. The crystalline form of carvedilol was changed into amorphous form after antisolvent precipitation. The dissolution rate of carvedilol was significantly accelerated by a reduction in particle size. The intestinal absorption of carvedilol nanosuspensions was greatly improved in comparison with microsuspensions and solution in the in situ single-pass perfusion experiment. The in vivo evaluation demonstrated that carvedilol nanosuspensions and microsuspensions exhibited markedly increased C max (2.09- and 1.48-fold) and AUC 0− t (2.11- and 1.51-fold), and decreased T max (0.34- and 0.48-fold) in contrast with carvedilol coarse suspensions. Moreover, carvedilol nanosuspensions showed good biocompatibility with the rat gastric mucosa in in vivo gastrointestinal irritation test. The entire results implicated that the dissolution rate and the oral absorption of carvedilol were significantly affected by the particle size. Particle size reduction to form nanosized particles was found to be an efficient method for improving the oral bioavailability of carvedilol.

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“…This could be explained by the Noyes-Whitney equation. 33,34 As when drug particles are smaller, the corresponding surface area is larger, so the nanoparticles provided a large increase in the surface area. Furthermore, according to the Prandtl equation, 35 the diffusion distance, h, decreases for very small particles.…”

mentioning

confidence: 99%

Process optimization and evaluation of novel baicalin solid nanocrystals

Yue¹,

Liu²,

Wan³

et al. 2013

IJN

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Effect of Crystal Size on the In Vitro Dissolution and Oral Absorption of Nitrendipine in Rats

Cited by 105 publications

References 40 publications

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation

Process optimization and evaluation of novel baicalin solid nanocrystals

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Effect of Crystal Size on the In Vitro Dissolution and Oral Absorption of Nitrendipine in Rats

Cited by 105 publications

References 40 publications

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Effects of polymer molecular weight on relative oral bioavailability of curcumin

Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in&nbsp;vivo&nbsp;evaluation

Process optimization and evaluation of novel baicalin solid nanocrystals

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Effect of particle size on oral absorption of carvedilol nanosuspensions: in vitro and in vivo evaluation