Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

Sun, Xiaoxiao; Wang, Nan; Yang, Li‐Ye; Ouyang, Xiaolong; Huang, Fangfang

doi:10.3390/pharmaceutics11090430

Cited by 58 publications

(42 citation statements)

References 35 publications

(35 reference statements)

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“…The result intuitively shows that the uptake of FA-AmCS-TPP nanoparticles by tumor cells was significantly higher than that of AmCS-TPP nanoparticles. This confirms that the introduction of FA into the carriers can increase the uptake rate by cancer cells, which is consistent with previous reports [65,66,67,68,69].…”

Section: Resultssupporting

confidence: 93%

Fabrication of Ion-Crosslinking Aminochitosan Nanoparticles for Encapsulation and Slow Release of Curcumin

Sun

Ying

et al. 2019

Pharmaceutics

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Curcumin (Cur) has anticancer activities but has poor stability, which can be improved using carrier materials. In this study, chitosan was aminated to increase the number of amino groups on its surface, modified with folic acid (FA), and then made into nanoparticles by ionic crosslinking. Owing to ion interaction, the negatively charged, non-toxic tripolyphosphate (TPP) interacted with the positively charged amino group on the aminated chitosan (AmCS) surface, producing FA-AmCS-TPP nanoparticles, which were then characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared spectrophotometry (FT-IR), and thermogravimetric analysis (TGA). Their small particle size (175.2 ± 0.99 nm) and good surface positive potential (+42.4 mV) are beneficial for carrying antitumor drugs. We subsequently investigated whether coating of Cur by AmCS allows slow drug release by FA-AmCS-TPP nanoparticles in different pH environments, and estimated the Cur loading efficiency (EE-Cur). Our results showed that the cumulative release rate of Cur at 48 h was 56.2%, and that the EE-Cur reached 94.26 ± 0.91% with nanoparticles composed of 0.10 g AmCS, 10.0 mg FA, 10.0 mg TPP, and 15.0 mg Cur. Additionally, cytotoxicity experiments showed that the Cur/FA-AmCS-TPP nanoparticles had good targeting ability for tumor cells. Therefore, the non-toxic targeted composite nanoparticles had potential as a new antitumor agent that can overcome the limitations of Cur.

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Section: Resultssupporting

confidence: 93%

Fabrication of Ion-Crosslinking Aminochitosan Nanoparticles for Encapsulation and Slow Release of Curcumin

Sun

Ying

et al. 2019

Pharmaceutics

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“…DDSs have the ability to improve the biological activity, enhance the therapeutic index or extend the biological half-life of drugs [ 2 , 3 ]. Various materials including microspheres, mesoporous, micro/nanoparticles, liposomes, micelles, and emulsions were developed as effective drug carriers [ 4 ]. Currently, a wide range of nanoparticles are being advanced to serve as potential carriers for delivering drugs in a controlled mode to specific-targeted sites in the human body [ 5 , 6 , 7 , 8 ].…”

Section: Introductionmentioning

confidence: 99%

Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

et al. 2021

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An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

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“…1,3,9 A substantial number of studies have reported the applications of MSNs as drug carriers, and the use of MSNs as drug carriers have been proven to be successful in vitro. [6][7][8][10][11][12] To the best of our knowledge, the efficacy of MSN carriers is decided by the structural features which determine the physicochemical properties of MSNs, including shape, size, pore characteristics, and surface chemistry. 13 Along with great progress in the structure control and multi-functionalization design of MSNs, various drug delivery formulations such as immediate drug delivery systems, sustained drug delivery systems, controlled drug delivery systems, targeted drug delivery systems, and stimuli-responsive drug delivery systems have been developed to improve the dissolution and bioavailability of poorly water-soluble drugs and enhance their therapeutic potential.…”

Section: Introductionmentioning

confidence: 99%

“…13 Along with great progress in the structure control and multi-functionalization design of MSNs, various drug delivery formulations such as immediate drug delivery systems, sustained drug delivery systems, controlled drug delivery systems, targeted drug delivery systems, and stimuli-responsive drug delivery systems have been developed to improve the dissolution and bioavailability of poorly water-soluble drugs and enhance their therapeutic potential. [9][10][11][12]14,15 It should be noted that, a slight change in structural features of MSNs may not only significantly influence their host-guest interactions with drug molecules, but also impact the biological binding ability with tissues and cells. 4,16 For example, Lu et al demonstrated that decreasing the size of NPs (from 50-280 nm) is an effective way to facilitate the cell uptake of MSNs.…”

Section: Introductionmentioning

confidence: 99%

<p>Superiority of L-tartaric Acid Modified Chiral Mesoporous Silica Nanoparticle as a Drug Carrier: Structure, Wettability, Degradation, Bio-Adhesion and Biocompatibility</p>

Hu¹,

Wang²,

Li³

et al. 2020

IJN

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Purpose: The purpose of this research was to study the basic physicochemical and biological properties regarding the application of L-tartaric acid modified chiral mesoporous silica nanoparticle (CMSN) as a drug carrier, and to explore the structure-property relationship of silica-based materials. Methods: CMSN with functions of carboxyl modification and chirality was successfully synthesized through co-condensation method, and the basic characteristics of CMSN, including morphology, structure, wettability, degradation, bio-adhesion and retention ability in gastrointestinal tract (GI tract) were estimated by comparing with non-functionalized mesoporous silica nanoparticles (MSN). Meanwhile, the biocompatibility and toxicity of L-tartaric modification were systematically evaluated both in vitro and in vivo through MTT cell viability assay, cell cycle and apoptosis assay, hemolysis assay, histopathology examination, hematology analysis, and clinical chemistry examination. Results: CMSN and MSN were spherical nanoparticles with uniform mesoporous structure. CMSN with smaller pore size and carboxyl functional groups exhibited better wettability. Besides, CMSN and MSN could dissolve thoroughly in simulated physiological fluids during a degradation period of 1-12 weeks. Interestingly, the in vitro and in vivo behaviors of carriers, including degradation, bio-adhesion and retention ability in the GI tract were closely related to wettability. As expected, CMSN had faster degradation rate, higher mucosa-adhesion ability, and longer retention time. Particularly, CMSN improved the bio-adhesion property in both gastric mucosa and small intestinal mucosa, and prolonged the GI tract retention time to at least 12 h, which meant higher probability for absorption. The biocompatibility and toxicity examination indicated that CMSN was a kind of biocompatible bio-material with good blood compatibility and negligible toxicity, which is required for further applications in biological fields. Conclusion: CMSN with functions of carboxyl modification and chirality had superiority in terms of both physicochemical and biological properties. The in vitro and in vivo behaviors of carriers, including degradation, bio-adhesion, and retention were closely related to wettability.

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Folic Acid and PEI Modified Mesoporous Silica for Targeted Delivery of Curcumin

Cited by 58 publications

References 35 publications

Fabrication of Ion-Crosslinking Aminochitosan Nanoparticles for Encapsulation and Slow Release of Curcumin

Fabrication of Ion-Crosslinking Aminochitosan Nanoparticles for Encapsulation and Slow Release of Curcumin

Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

<p>Superiority of L-tartaric Acid Modified Chiral Mesoporous Silica Nanoparticle as a Drug Carrier: Structure, Wettability, Degradation, Bio-Adhesion and Biocompatibility</p>

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