Preparation, characterization, biodistribution and antitumor efficacy of hydroxycamptothecin nanosuspensions

Han, Meihua; Liu, Xiaoli; Guo, Yifei; Wang, Yanhong; Wang, Xiangtao

doi:10.1016/j.ijpharm.2013.07.056

Cited by 40 publications

(38 citation statements)

References 32 publications

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“…Nanoparticles (NPs) in general have many properties that are different from those of traditionally used materials [10,[17][18][19][20][21][22][23][24][25][26][27][28]. They have dimensions typically below 100 nm, which allows them to reach specific sites inside the body and even to be permeable to tissues and cells.…”

Section: Antimicrobial Approaches Based On Nanotechnologymentioning

confidence: 99%

Magnetite Nanostructures as Novel Strategies for Anti-Infectious Therapy

2014

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Abstract:This review highlights the current situation of antimicrobial resistance and the use of magnetic nanoparticles (MNPs) in developing novel routes for fighting infectious diseases. The most important two directions developed recently are: (i) improved delivery of antimicrobial compounds based on a drastic decrease of the minimal inhibition concentration (MIC) of the drug used independently; and (ii) inhibition of microbial attachment and biofilm development on coated medical surfaces. These new directions represent promising alternatives in the development of new strategies to eradicate and prevent microbial infections that involve resistant and biofilm-embedded bacteria. Recent promising applications of MNPs, as the development of delivery nanocarriers and improved nanovehicles for the therapy of different diseases are discussed, together with the mechanisms of microbial inhibition.

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Section: Antimicrobial Approaches Based On Nanotechnologymentioning

confidence: 99%

Magnetite Nanostructures as Novel Strategies for Anti-Infectious Therapy

2014

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“…Nearly all the reported nanocrystals presented with a regular crystalline shape or irregular fragment due to powerful grinding or homogenization of the original crystal drugs by top-down method; however, the HCPT-NSps had a uniform near-spherical shape. The drug in nanosuspensions that were prepared by solvent precipitation method was basically in an amorphous state; 26,28 this study presents an unusual case.…”

Section: Xrd Measurementmentioning

confidence: 90%

“…Figure 2B shows a TEM micrograph of the HCPT-NSps. The TEM micrograph indicated that the nanosuspensions were smaller than observed by DLS examination due to particle shrinkage caused by the drying process, 28 and all the nanosuspensions had a near-spherical shape with minor deformation. In the micrograph, small dark punctated spots that were formed due to phosphotungstic acid staining were observed.…”

mentioning

confidence: 86%

“…In most cases, a considerable number of cryoprotectants are required to maintain the structure of the nanoparticles and avoid adhesion or aggregation during lyophilization. 21,26,28 Thus, the lyophilized powder particles become nanoparticles upon being resuspended in water. However, addition of various cryoprotectants will further decrease the actual drug-loading content of the nanoparticles in the final product and causes inconvenience, especially when a large clinical dose is required.…”

Section: Lyophilization and Stability Testmentioning

confidence: 99%

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10-Hydroxycamptothecin (HCPT) nanosuspensions stabilized by mPEG<sub>1000</sub>-HCPT conjugate: high stabilizing efficiency and improved antitumor efficacy

Yang¹,

Hong²,

Jiang³

et al. 2017

IJN

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In this study, polyethylene glycol (PEG)ylated 10-hydroxycamptothecin (mPEG 1000 -HCPT) was synthesized and used as a stabilizer to prepare 10-hydroxycamptothecin (HCPT) nanosuspensions for their in vitro and in vivo antitumor investigation. The resultant HCPT nanosuspensions (HCPT-NSps) had a very high drug payload of 94.90% (w/w) and a mean particle size of 92.90±0.20 nm with narrow size distribution (polydispersity index of 0.16±0.01). HCPT-NSps could be lyophilized without the need of the addition of any cryoprotectant and then be reconstituted into nanosuspensions of a similar size by direct resuspension in water. HCPT was in crystalline form in HCPT-NSps. Using mPEG 1000 -HCPT as stabilizer, insoluble camptothecin and 7-ethyl-10-hydroxycamptothecin could also be easily made into nanosuspensions with similar features such as high drug payload, small particle size, and cryoprotectant-free freeze drying. The 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide assay indicated that the HCPT-NSps had a significantly higher cytotoxicity than HCPT injections, with 3.77 times lower IC 50 value against HepG2 cells and 14.1 times lower IC 50 value against MCF-7 cells. An in vivo study in H22 tumor-bearing mice after intravenous injection of HCPT-NSps demonstrated that HCPT-NSps significantly improved the antitumor efficacy compared to the commercially available HCPT injections (86.38% vs 34.97%) at the same dose of 5 mg/kg. Even at 1/4 of the dose, HCPT-NSps could also achieve a similar antitumor efficacy to that of HCPT injections. mPEG 1000 -HCPT may be a highly efficient stabilizer able to provide camptothecin-based drugs, and probably other antitumor agents containing aromatic structure, with unique nanosuspensions or nanocrystals for improved in vivo therapeutic efficacy.

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“…The highest fluorescence intensity was found in the liver and then in the spleen, which was in accordance with previously studies. [42][43][44] NSps may be recognized as foreign objects by the immune system when entering the blood circulation and then may be partially uptaken by phagocytic cells of the mononuclear phagocyte system which abounded in special tissues and organs, such as the liver and spleen. 42 The FA-ACGs-NSps group displayed much more fluorescence in the tumor than the ACGs-NSps group (P,0.05, Figure 7B), but pretreatment with free FA caused a significant reduction (as observed in the FA inhibition group, P,0.05).…”

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confidence: 99%

Folate-modified Annonaceous acetogenins nanosuspensions and their improved antitumor efficacy

Hong

Sun

et al. 2017

IJN

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Annonaceous acetogenins (ACGs) are a large family of fatty acid derived natural products that are exclusively isolated from the Annonaceae species. Many members of this diverse family have a broad spectrum of biological activities, the most impressive of which is anticancer activity. However, their poor solubility and severe toxicity restrict their clinical application, and their complicated composition hinders their formulation and drug delivery. In this study, β-cyclodextrin was modified with folic acid (FA) and then combined with soybean lecithin to prepare FA-modified ACGs nanosuspensions (FA-ACGs-NSps). The obtained FA-ACGs-NSps had a high drug payload of 57.59% and average particle size of 199.5 nm, and they exhibited sustained drug release within 142 hours. In comparison with ACGs-NSps, FA-ACGs-NSps showed significantly enhanced cytotoxicity and higher cell uptake toward folate receptor-positive 4T1 cell lines. An in vivo study demonstrated that FA-ACGs-NSps more effectively accumulated in tumors and enhanced the antitumor therapeutic efficacy with less toxicity in 4T1 tumor bearing mice. Therefore, FA-ACGs-NSps may be a promising drug delivery system for ACGs to improve their therapeutic window and may be suitable for clinical application to treat folate-positive tumors.

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Preparation, characterization, biodistribution and antitumor efficacy of hydroxycamptothecin nanosuspensions

Cited by 40 publications

References 32 publications

Magnetite Nanostructures as Novel Strategies for Anti-Infectious Therapy

Magnetite Nanostructures as Novel Strategies for Anti-Infectious Therapy

10-Hydroxycamptothecin (HCPT) nanosuspensions stabilized by mPEG<sub>1000</sub>-HCPT conjugate: high stabilizing efficiency and improved antitumor efficacy

Folate-modified Annonaceous acetogenins nanosuspensions and their improved antitumor efficacy

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