Folate and TAT Peptide Co-Modified Liposomes Exhibit Receptor-Dependent Highly Efficient Intracellular Transport of Payload In Vitro and In Vivo

Zhu, Yueyong; Cheng, Liang; Liu, Cheng; Huang, Fa-Zhen; Hu, Qing; Li, Ling; Tian, Chenmin; Lin, Wei; Chen, Fan

doi:10.1007/s11095-014-1418-z

Cited by 30 publications

(17 citation statements)

References 39 publications

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“…The solvent was then dialyzed against demonized water using a membrane with MW cutoff (MWCO) of 13 kDa for 24 h. The product was then lyophilized for use. The reaction progress was monitored by thin-layer chromatography (TLC) 23. TLC confirmed the formation of TAT-PEG-PLGA as the spot of PLGA-PEG-Mal disappeared after the reaction.…”

Section: Methodsmentioning

confidence: 99%

A novel local anesthetic system: transcriptional transactivator peptide-decorated nanocarriers for skin delivery of ropivacaine

Chen¹,

You²

2017

DDDT

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PurposeBarrier properties of the skin and physicochemical properties of drugs are the main factors for the delivery of local anesthetic molecules. The present work evaluates the anesthetic efficacy of drug-loaded nanocarrier (NC) systems for the delivery of local anesthetic drug, ropivacaine (RVC).MethodsIn this study, transcriptional transactivator peptide (TAT)-decorated RVC-loaded NCs (TAT-RVC/NCs) were successfully fabricated. Physicochemical properties of NCs were determined in terms of particle size, zeta potential, drug encapsulation efficiency, drug-loading capacity, stability, and in vitro drug release. The skin permeation of NCs was examined using a Franz diffusion cell mounted with depilated mouse skin in vitro, and in vivo anesthetic effect was evaluated in mice.ResultsThe results showed that TAT-RVC/NCs have a mean diameter of 133.2 nm and high drug-loading capacity of 81.7%. From the in vitro skin permeation results, it was observed that transdermal flux of TAT-RVC/NCs was higher than that of RVC-loaded NCs (RVC/NCs) and RVC injection. The evaluation of in vivo anesthetic effect illustrated that TAT-RVC/NCs can enhance the transdermal delivery of RVC by reducing the pain threshold in mice.ConclusionThese results indicate that TAT-decorated NCs systems are useful for overcoming the barrier function of the skin, decreasing the dosage of RVC and enhancing the anesthetic effect. Therefore, TAT-decorated NCs can be used as an effective transdermal delivery system for local anesthesia.

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Section: Methodsmentioning

confidence: 99%

A novel local anesthetic system: transcriptional transactivator peptide-decorated nanocarriers for skin delivery of ropivacaine

Chen¹,

You²

2017

DDDT

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“…Doxorubicin liposomes were prepared by the pH gradient method with modifications (Zhu et al, 2014). Briefly, DOTAP/cy5:DPPC:DOPE:Cholesterol:DSPE-PEG 2000 (5:20:5:4:2.5) weight ratio were dissolved in 200 μl of ethanol and heated in a water bath to a temperature range of 50–60°C to constitute the organic phase.…”

Section: Methodsmentioning

confidence: 99%

Doxorubicin liposomes as an investigative model to study the skin permeation of nanocarriers

Boakye

Patel

Singh

2015

International Journal of Pharmaceutics

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The objectives of this study were to develop an innovative investigative model using doxorubicin as a fluorophore to evaluate the skin permeation of nanocarriers and the impact of size and surface characteristics on their permeability. Different doxorubicin-loaded liposomes with mean particle size <130nm and different surface chemistry were prepared by ammonium acetate gradient method using DPPC, DOPE, Cholesterol, DSPE-PEG 2000 and 1,1-Di-((Z)-octadec-9-en-1-yl)pyrrolidin-1-ium chloride (CY5)/DOTAP/1,2-dioleoyl-sn-glycero-3-phosphate (DOPA) as the charge modifier. There was minimal release of doxorubicin from the liposomes up to 8 h; indicating that fluorescence observed within the skin layers was due to the intact liposomes. Liposomes with particle sizes >600nm were restricted within the stratum corneum. DOTAP (p<0.01) and CY5 (p<0.05) liposomes demonstrated significant permeation into the skin than DOPA and PEG liposomes. Tape stripping significantly (p<0.01) enhanced the skin permeation of doxorubicin liposomes but TAT-decorated doxorubicin liposomes permeated better (p<0.005). Blockage of the hair follicles resulted in significant reduction in the extent and intensity of fluorescence observed within the skin layers. Overall, doxorubicin liposomes proved to be an ideal fluorophore-based model. The hair follicles were the major route utilized by the liposomes to permeate skin. Surface charge and particle size played vital roles in the extent of permeation.

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“…For example, transactivating transcriptional activator peptide (Tat) is a wellknown cell-penetrating peptide (CPP), which can enhance the efficient uptake of nanocarriers by target cells. Therefore, the combination of FR-mediated specificity and CPPmediated penetration may increase the efficiency of current FA-targeted nanocarriers for cancer therapy [163]. Dual targeting through FA and some anti-tumor antigen monoclonal antibodies is another approach in improving tumor sitespecific cancer therapy.…”

Section: Resultsmentioning

confidence: 99%

Folate-conjugated nanoparticles as a potent therapeutic approach in targeted cancer therapy

et al. 2015

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The selective and efficient drug delivery to tumor cells can remarkably improve different cancer therapeutic approaches. There are several nanoparticles (NPs) which can act as a potent drug carrier for cancer therapy. However, the specific drug delivery to cancer cells is an important issue which should be considered before designing new NPs for in vivo application. It has been shown that cancer cells over-express folate receptor (FR) in order to improve their growth. As normal cells express a significantly lower levels of FR compared to tumor cells, it seems that folate molecules can be used as potent targeting moieties in different nanocarrier-based therapeutic approaches. Moreover, there is evidence which implies folate-conjugated NPs can selectively deliver anti-tumor drugs into cancer cells both in vitro and in vivo. In this review, we will discuss about the efficiency of different folate-conjugated NPs in cancer therapy.

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Folate and TAT Peptide Co-Modified Liposomes Exhibit Receptor-Dependent Highly Efficient Intracellular Transport of Payload In Vitro and In Vivo

Abstract: Folate and TAT peptide co-modified liposome using different chain lengths of PEG as linkers may provide a useful strategy for specific and efficient intracellular drug delivery.

Cited by 30 publications

References 39 publications

A novel local anesthetic system: transcriptional transactivator peptide-decorated nanocarriers for skin delivery of ropivacaine

A novel local anesthetic system: transcriptional transactivator peptide-decorated nanocarriers for skin delivery of ropivacaine

Doxorubicin liposomes as an investigative model to study the skin permeation of nanocarriers

Folate-conjugated nanoparticles as a potent therapeutic approach in targeted cancer therapy

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