pH-sensitive properties of surface charge-switched multifunctional polymeric micelle

Oh, Kyung Taek; Kim, Dongin; You, Han; Ahn, Yong Sik; Lee, Eun Seong

doi:10.1016/j.ijpharm.2009.04.021

Cited by 54 publications

(19 citation statements)

References 37 publications

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“…Oh and Lee recently developed poly(Lys) based pH-sensitive carriers (Oh et al 2009b;Oh et al 2009c). A micellar system (particle size: ~165 nm) constructed from poly(N…”

Section: Polypeptide Block Copolymersmentioning

confidence: 99%

“…The systems using DOX as the model drug showed acceleration of DOX release from the micelles in response to tumor pH e (Oh et al 2009c). In addition, a surface chargeswitched polymeric micelle with a pH signal was developed as a drug-carrying nanovehicle for tumor targeting (Oh et al 2009b). The micelles (particle size: ~85 nm), constructed from PLA-b-PEG-b-poly(L-lysine-Nε-(2,3-dimethyl maleic acid)) [poly(Lys)-DMA] and formed by self-assembly in an aqueous pH 7.4 solution, consisted of a hydrophobic core (PLA core) and two hydrophilic shells [PEG shell and Poly(Lys)-DMA shell] (Oh et al 2009b).…”

Section: Polypeptide Block Copolymersmentioning

confidence: 99%

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Functional Polymers for Drug Delivery Systems in Nanomedicines

Lee¹,

Kim²,

Yun³

et al. 2010

Journal of Pharmaceutical Investigation

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− Polymeric based nanomedicines have been developed for diagnosing, treating, and preventing diseases in human body. The nanosized drug delivery systems having various structures such as micelles, nanogels, drug-conjugates, and polyplex were investigated for a great goal in pharmaceutics: increasing therapeutic efficacy for diseases and decreasing drug toxicity for normal tissues. The functional polymers used for constituting these drug delivery systems should have several favorable properties such as stimuli-responsibility and biodegrdability for controlled drug release, and solublization capacity for programmed drug encapsulation. This review discusses recent developments and trends of functional polymers (e.g., pH-sensitive polymers, biodegradable polymers, and cationic polymers) used for nanosized drug carriers.

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“…Oh and Lee recently developed poly(Lys) based pH-sensitive carriers (Oh et al 2009b;Oh et al 2009c). A micellar system (particle size: ~165 nm) constructed from poly(N…”

Section: Polypeptide Block Copolymersmentioning

confidence: 99%

Section: Polypeptide Block Copolymersmentioning

confidence: 99%

Functional Polymers for Drug Delivery Systems in Nanomedicines

Lee¹,

Kim²,

Yun³

et al. 2010

Journal of Pharmaceutical Investigation

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“…It is useful and important for chemotherapy of cancers in pH-sensitive delivery system. The pH sensitivity could enhance the release of anticancer drugs at the triggering lower pH of endosomes or lysosomes in cytoplasm that could reduce the side cytotoxicity and enhance the efficacy of anticancer drugs (Bae et al, 2005b;Ganta et al, 2008;Oh et al, 2009). As known, the polymer micelles are good vehicles for the poorly soluble anticancer drugs within the core-shell structure.…”

Section: Introductionmentioning

confidence: 99%

Dual thermoresponsive and pH-responsive self-assembled micellar nanogel for anticancer drug delivery

Chen

Sun

et al. 2013

Drug Delivery

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In this article, we prepared a dual thermoresponsive and pH-responsive self-assembled micellar nanogel for anticancer drug delivery by using a degradable pH-responsive ketal derivative, mPEG2000-Isopropylideneglycerol (mPEG-IS, PI) polymer. The purpose of this study is to develop an injectable dual-responsive micellar nanogel system which has a sol-gel phase transition by the stimulation of body temperature with improved stability and biocompatibility as a controlled drug delivery carrier for cancer therapy. The pH-responsive PI was designed with pH-responsive ketal group as hydrophobic moieties and PEG group as hydrophilic moieties. The PI micelles encapsulated paclitaxel (PTX) was fabricated. Then, the PI micelles were formed in a thermo-nanogel. The micellar nanogel could improve the solubility and stability of PTX. The physiochemical properties of PI micelles and micellar nanogel were characterized. The results showed that dual-responsive micellar nanogel could carry out sol-gel transition at 37 C. The PI polymer can spontaneously self-assemble into micellar structure with size of 100-200 nm. The dual-responsive micellar nanogel could be degraded under lower pH condition. The test in vitro PTX release showed that dual-responsive micellar nanogel could release about 70% for 70 h under pH 5.0 while about 10% release at pH 7.4 and pH 9.0. The dual-responsive micellar nanogel was of lower cytotoxicity and suppressed tumor growth most efficiently. The micellar nanogel will be a new potential dual-responsive drug delivery system for cancer therapy.

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“…18,19 Although PAA can easily be functionalized to respond to external stimuli (such as light, heat, and acid), in vivo application of the drug carrier is greatly limited due to its non-biodegradability. Compared to PAA, poly(amino acid)s such as poly(Lglutamic acid) (PGA), 20,21 poly(L-aspartic acid), 17,22 and poly(L-lysine) 17,22,23 have better in vivo biocompatibility and biodegradability, and bear reactive side carboxyl or primary amine groups that can easily be modified to confer stimuli-responsive capabilities. Moreover, as an available acid-responsive polypeptide, PGA could undergo a sharp-phase transition by helix-coil conformational change to significantly benefit the accelerative release of the entrapped drug, once the pH value is close to or below its pK a (#4.25).…”

Section: Introductionmentioning

confidence: 99%

Acid-triggered core cross-linked nanomicelles for targeted drug delivery and magnetic resonance imaging in liver cancer cells

Li¹,

Li²,

Yi³

et al. 2013

IJN

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Purpose:To research the acid-triggered core cross-linked folate-poly(ethylene glycol)-b-poly [N-(N′,N′-diisopropylaminoethyl) glutamine] (folated-PEG-P[GA-DIP]) amphiphilic block copolymer for targeted drug delivery and magnetic resonance imaging (MRI) in liver cancer cells. Methods:As an appropriate receptor of protons, the N,N-diisopropyl tertiary amine group (DIP) was chosen to conjugate with the side carboxyl groups of poly(ethylene glycol)-b-poly (L-glutamic acid) to obtain PEG-P(GA-DIP) amphiphilic block copolymers. By ultrasonic emulsification, PEG-P(GA-DIP) could be self-assembled to form nanosized micelles loading doxorubicin (DOX) and superparamagnetic iron oxide nanoparticles (SPIONs) in aqueous solution. When PEG-P(GA-DIP) nanomicelles were combined with folic acid, the targeted effect of folated-PEG-P(GA-DIP) nanomicelles was evident in the fluorescence and MRI results. Results: To further increase the loading efficiency and the cell-uptake of encapsulated drugs (DOX and SPIONs), DIP (pK a ≈6.3) groups were linked with ∼50% of the side carboxyl groups of poly(L-glutamic acid) (PGA), to generate the core cross-linking under neutral or weakly acidic conditions. Under the acidic condition (eg, endosome/lysosome), the carboxyl groups were neutralized to facilitate disassembly of the P(GA-DIP) blocks' cross-linking, for duly accelerating the encapsulated drug release. Combined with the tumor-targeting effect of folic acid, specific drug delivery to the liver cancer cells and MRI diagnosis of these cells were greatly enhanced. Conclusion: Acid-triggered and folate-decorated nanomicelles encapsulating SPIONs and DOX, facilitate the targeted MRI diagnosis and therapeutic effects in tumors.

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pH-sensitive properties of surface charge-switched multifunctional polymeric micelle

Cited by 54 publications

References 37 publications

Functional Polymers for Drug Delivery Systems in Nanomedicines

Functional Polymers for Drug Delivery Systems in Nanomedicines

Dual thermoresponsive and pH-responsive self-assembled micellar nanogel for anticancer drug delivery

Acid-triggered core cross-linked nanomicelles for targeted drug delivery and magnetic resonance imaging in liver cancer cells

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