Synthesis of VIP-Lipopeptide Using a New Linker to Modify Liposomes: Towards the Development of a Drug Delivery System for Active Targeting

Masaka, Toru; Matsuda, Takuya; Li, Yingpeng; Koide, Yuki; Takami, Akira; Yano, Kenji; Imai, Ryōsuke; Ichihara, Risa; Yagi, Nobuhiro; Suzuki, Hideharu; Hikawa, Hidemasa; Terada, Katsuhide; Yokoyama, Yuusaku

doi:10.1248/cpb.c13-00518

Cited by 3 publications

(2 citation statements)

References 19 publications

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“…With the use of new technology and equipment, and the development and application of excellent carrier materials and accessories, targeted drug delivery (TDD) technology has been developing rapidly in recent years, and has gradually extended to the treatment fields of multiple diseases ( 14 – 17 ).…”

Section: Discussionmentioning

confidence: 99%

Preparation of a liposomal delivery system and its in vitro release of rapamycin

Miao

Deng

et al. 2015

Experimental and Therapeutic Medicine

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The aim of this study was to prepare a liposomal delivery system for rapamycin and study its in vitro release characteristics. The results may provide a foundation for the further development of a liposomal delivery system for rapamycin and the establishment of a new active treatment method targeted towards the cellular components of atherosclerotic plaques. The ethanol injection method was used to prepare rapamycin-containing liposomes. The formulation was optimized by orthogonal design, and the degree of rapamycin release by the liposomes was measured by the reverse dialysis method. Orthogonal testing showed that the optimum formulation had a phospholipid concentration of 4%, a phospholipid-cholesterol mass ratio of 8:1, a drug-lipid mass ratio of 1:20 and an aqueous phase pH of 7.4. Rapamycin-containing liposomes with an encapsulation efficiency of 82.11±2.13% were prepared, and the in vitro release of rapamycin from the liposomes complied with a first-order kinetic equation. In conclusion, the formulation was optimized, the prepared liposomes had a high rapamycin encapsulation rate and good reproducibility, and their in vitro release had a certain delayed-release effect.

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Section: Discussionmentioning

confidence: 99%

Preparation of a liposomal delivery system and its in vitro release of rapamycin

Miao

Deng

et al. 2015

Experimental and Therapeutic Medicine

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show abstract

“…With the use of new technology and equipment, as well as the development and application of excellent carrier materials and accessories, targeted drug delivery technology has been developing rapidly in recent years, and has gradually extended to the treatment of a number of diseases. 17 – 20 Liposomes have been extensively researched as targeted drug delivery carriers, and been found to have sustained-release properties, long-lasting effects, low systemic toxicity, and good biocompatibility, and to be suitable for administration by a number of routes. Traditional liposomes only had a passive targeting role; however, if antibody or ligand molecules targeted to proliferating intimal tissues can be connected to the liposomal membrane to form targeted liposomes, active targeting could be achieved.…”

Section: Resultsmentioning

confidence: 99%

RGD-modified liposomes enhance efficiency of aclacinomycin A delivery: evaluation of their effect in lung cancer

Feng¹,

Li²,

Dong³

et al. 2015

DDDT

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In this study, long-circulating Arg-Gly-Asp (RGD)-modified aclacinomycin A (ACM) liposomes were prepared by thin film hydration method. Their morphology, particle size, encapsulation efficiency, and in vitro release were investigated. The RGD-ACM liposomes was about 160 nm in size and had the visual appearance of a yellowish suspension. The zeta potential was −22.2 mV and the encapsulation efficiency was more than 93%. The drug-release behavior of the RGD-ACM liposomes showed a biphasic pattern, with an initial burst release and followed by sustained release at a constant rate. After being dissolved in phosphate-buffered saline (pH 7.4) and kept at 4°C for one month, the liposomes did not aggregate and still had the appearance of a milky white colloidal solution. In a pharmacokinetic study, rats treated with RGD-ACM liposomes showed slightly higher plasma concentrations than those treated with ACM liposomes. Maximum plasma concentrations of RGD-ACM liposomes and ACM liposomes were 4,532 and 3,425 ng/mL, respectively. RGD-ACM liposomes had a higher AUC0–∞ (1.54-fold), mean residence time (2.09-fold), and elimination half-life (1.2-fold) when compared with ACM liposomes. In an in vivo study in mice, both types of liposomes inhibited growth of human lung adenocarcinoma (A549) cells and markedly decreased tumor size when compared with the control group. There were no obvious pathological tissue changes in any of the treatment groups. Our results indicate that RGD-modified ACM liposomes have a better antitumor effect in vivo than their unmodified counterparts.

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Liposome Modified with VIP-Lipopeptide as a New Drug Delivery System

Masaka

Li²,

Kawatobi³

et al. 2014

YAKUGAKU ZASSHI

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We have designed a novel lipid analog (lipopeptide) that mimics the structural features of modiˆed phospholipids. This lipopeptide is easily synthesized using a peptide synthesizer and has been shown to be useful for the modiˆcation of liposomes, which are used as an active targeted drug delivery system (DDS). Vasoactive intestinal peptide (VIP) has high homology with pituitary adenylate cyclase activating peptide (PACAP). There are three major PACAP receptors: PAC1R, VPAC1R, and VPAC2R. PAC1R has a‹nity only for PACAP, whereas VPAC1R and VPAC2R have the same a‹nity for both VIP and PACAP. In the present study, we synthesized several lipopeptides conjugated with VIP through diŠerent linkers and found that liposomes modiˆed with these lipopeptides (VIP-Lips) selectively recognized the PACAP/VIP receptors. The anti-cancer activity of these VIP-Lips was evaluated by encapsulation of an antitumor drug, doxorubicin (DOX), into the modiˆed liposomes (VIP-Lips-DOX) against the human osteosarcoma cell line, Saos-2, which highly expresses the VIP receptor. cAMP production was then measured to determine how well the VIPLips were able to recognize VPAC2R. The results clearly indicate that the proposed lipopeptide methodology holds promise as a DDS for cancer therapy.

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Synthesis of VIP-Lipopeptide Using a New Linker to Modify Liposomes: Towards the Development of a Drug Delivery System for Active Targeting

Cited by 3 publications

References 19 publications

Preparation of a liposomal delivery system and its in vitro release of rapamycin

Preparation of a liposomal delivery system and its in vitro release of rapamycin

RGD-modified liposomes enhance efficiency of aclacinomycin A delivery: evaluation of their effect in lung cancer

Liposome Modified with VIP-Lipopeptide as a New Drug Delivery System

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Synthesis of VIP-Lipopeptide Using a New Linker to Modify Liposomes: Towards the Development of a Drug Delivery System for Active Targeting

Cited by 3 publications

References 19 publications

Preparation of a liposomal delivery system and its in vitro release of rapamycin

Preparation of a liposomal delivery system and its in vitro release of rapamycin

RGD-modified liposomes enhance efficiency of&nbsp;aclacinomycin A delivery: evaluation of their effect in lung cancer

Liposome Modified with VIP-Lipopeptide as a New Drug Delivery System

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RGD-modified liposomes enhance efficiency of aclacinomycin A delivery: evaluation of their effect in lung cancer