Preparation, characterization of hydrophilic and hydrophobic drug in combine loaded chitosan/cyclodextrin nanoparticles and in vitro release study

Ji, Jingou; Hao, Shilei; Liu, Weiqi; Dan-jun, Wu; Wang, Tengfei; Xu, Yanhua

doi:10.1016/j.colsurfb.2010.11.005

Cited by 144 publications

(55 citation statements)

References 26 publications

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“…The observed initial burst release of MTX from the NPs might be due to drug molecules that were loosely incorporated into them, e.g., by electrostatic interaction between the positively charged amino groups of CS in the particle surface and the ionized carboxyl groups of MTX. At physiological pH, we obtained a relatively slow release up to 24 h, which could be attributed to drug diffusion and the swelling/degradation of the polymer [40]. In contrast, the release rate was accelerated by decreasing pH, which confirms the pH-dependent release pattern of this nanoarchitecture.…”

Section: Discussionsupporting

confidence: 58%

In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles

et al. 2013

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Nanoparticles with pH-sensitive behavior may enhance the success of chemotherapy in many cancers by efficient intracellular drug delivery. Here, we investigated the effect of a bioactive surfactant with pH-sensitive properties on the antitumor activity and intracellular behavior of methotrexate-loaded chitosan nanoparticles (MTX-CS-NPs). NPs were prepared using a modified ionotropic complexation process, in which was included the surfactant derived from N α ,N ε -dioctanoyl lysine with an inorganic lithium counterion. The pH-sensitive behavior of NPs allowed accelerated release of MTX in an acidic medium, as well as membrane-lytic pH-dependent activity, which facilitated the cytosolic delivery of endocytosed materials. Moreover, our results clearly proved that MTX-CS-NPs were more active against the tumor HeLa and MCF-7 cell lines than the free drug. The feasibilty of using NPs to target acidic tumor extracellular pH was also shown, as cytotoxicity against cancer cells was greater in a mildly acidic environment. Finally, the combined physicochemical and pH-sensitive properties of NPs generally allowed the entrapped drug to induce greater cell cycle arrest and apoptotic effects. Therefore, our overall results suggest that pH-sensitive MTX-CS-NPs could be potentially useful as a carrier system for tumor and intracellular drug delivery in cancer therapy.

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Section: Discussionsupporting

confidence: 58%

In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles

et al. 2013

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“…The WAXS patterns corresponding to the pure MTX (Figure 2a) exhibited several strong scattering peaks of lower and higher intensities, demonstrating the crystalline nature of the MTX. The WAXS pattern of MTX was similar to that previously reported (Jingou et al, 2011). The WAXS recorded for PCL (Figure 2b) demonstrated two characteristic peaks between 20 and 25 , confirming its semi-crystalline structure (Wang & Gou, 2008), and a series of peaks above 20…”

Section: Characterizationsupporting

confidence: 66%

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Pereira

Barbosa

et al. 2013

Drug Delivery

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Context: Methotrexate (MTX) is used in the treatment of malignancies; however, its clinical application is limited by its toxic dose-related side effects. An alternative to overcome the toxicity of the MTX in healthy tissues is the design of an implantable device capable of controlling the delivery of this drug for an extended period within the tumor site. Objective: To develop methotrexate-loaded poly("-caprolactone) implants (MTX PCL implants) and to demonstrate their efficacy as local drug delivery systems capable of inhibiting Ehrlich solid tumor bearing mice. Materials and methods: MTX PCL implants were produced by the melt-molding technique and were characterized by FTIR, WAXS, DSC and SEM. The in vitro and in vivo release of MTX from the PCL implants was also evaluated. The efficacy of implants in inhibiting tumor cells in culture and the solid tumor in a murine model was revealed. Results and discussion: The chemical and morphological integrity of the drug was preserved into the polymeric matrix. The in vitro and in vivo release processes of the MTX from the PCL implants were modulated by diffusion. MTX diffused from the implants revealed an antiproliferative effect on tumor cells. Finally, MTX controlled and sustained released from the polymeric implants efficiently reduced 42.7% of the solid tumor in mice paw. Conclusion: These implantable devices represented a contribution to improve the efficacy and safety of chemotherapy treatments, promoting long-term local drug accumulation in the targeted site.

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“…The main reason could be attributed to the difficulty in realization and control of co-loading in the mesoporous channels. Polymer nanoparticles and liposomes have also been used for delivery of hydrophobic and hydrophilic anticancer drugs; 34 however, chemical conjugation was generally involved in the loading processes, therefore increasing the operational complexity. Meanwhile, the stoichiometry issue is another obstacle to control the dose ratio.…”

Section: Introductionmentioning

confidence: 99%

Delivering hydrophilic and hydrophobic chemotherapeutics simultaneously by magnetic mesoporous silica nanoparticles to inhibit cancer cells

Liu¹,

Zhang²,

Sun³

et al. 2012

IJN

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Using nanoparticles to deliver chemotherapeutics offers new opportunities for cancer therapy, but challenges still remain when they are used for the delivery of multiple drugs, especially for the synchronous delivery of hydrophilic and hydrophobic drugs in combination therapies. In this paper, we developed an approach to deliver hydrophilic-hydrophobic anticancer drug pairs by employing magnetic mesoporous silica nanoparticles (MMSNs). We prepared 50 nm-sized MMSNs with uniform pore size and evaluated their capability for the loading of two combinations of chemotherapeutics, namely doxorubicin-paclitaxel and doxorubicinrapamycin, by means of sequential adsorption from the aqueous solution of doxorubicin and nonaqueous solutions of paclitaxel or rapamycin. Experimental results showed that the present strategy successfully realized the co-loading of hydrophilic and hydrophobic drugs with high-loading content and widely tunable ratio range. We elaborate on the theory behind the molecular interaction between the silica hydroxyl groups and drug molecules, which underlie the controllable loading, and the subsequent release of the drug pairs. Then we demonstrate that the multidrug-loaded MMSNs could be easily internalized by A549 human pulmonary adenocarcinoma cells, and produce enhanced tumor cell apoptosis and growth inhibition as compared to single-drug loaded MMSNs. Our study thus realized simultaneous and dose-tunable delivery of hydrophilic and hydrophobic drugs, which were endowed with improved anticancer efficacy. This strategy could be readily extended to other chemotherapeutic combinations and might have clinically translatable significance.

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Preparation, characterization of hydrophilic and hydrophobic drug in combine loaded chitosan/cyclodextrin nanoparticles and in vitro release study

Cited by 144 publications

References 26 publications

In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles

In vitro antitumor activity of methotrexate via pH-sensitive chitosan nanoparticles

Efficacy of methotrexate-loaded poly(ε-caprolactone) implants in Ehrlich solid tumor-bearing mice

Delivering hydrophilic and hydrophobic chemotherapeutics simultaneously by magnetic mesoporous silica nanoparticles to inhibit cancer cells

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