PEGylation and Cell-Penetrating Peptides: Glimpse into the Past and Prospects in the Future

2020 ◽  
Vol 20 (5) ◽  
pp. 337-348 ◽  
Author(s):  
Sumit Kumar ◽  
Devender Singh ◽  
Pooja Kumari ◽  
Rajender Singh Malik ◽  
Poonam ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Target ◽  
Pharmacokinetic Profile ◽  
Cell Penetrating Peptides ◽  
Physiochemical Properties ◽  
Drug Molecules ◽  
Pharmacokinetic Properties ◽  
Cell Penetrating

Several drug molecules have shown low bioavailability and pharmacokinetic profile due to metabolism by enzymes, excretion by the renal system, or due to other physiochemical properties of drug molecules. These problems have resulted in the loss of efficacy and the gain of side effects associated with drug molecules. PEGylation is one of the strategies to overcome these pharmacokinetic issues and has been successful in the clinic. Cell-penetrating Peptides (CPPs) help to deliver molecules across biological membranes and could be used to deliver cargo selectively to the intracellular site or to the drug target. Hence CPPs could be used to improve the efficacy and selectivity of the drug. However, due to the peptidic nature of CPPs, they have a low pharmacokinetic profile. Using PEGylation and CPPs together as a component of a drug delivery system, the and efficacy of drug molecules could be improved. The other important pharmacokinetic properties such as short half-life, solubility, stability, absorption, metabolism, and elimination could be also improved. Here in this review, we summarized PEGylated CPPs or PEGylation based formulations for CPPs used in a drug delivery system for several biomedical applications until August 2019.

scholarly journals Cell-penetrating Peptides as a Novel Transdermal Drug Delivery System

2012 ◽  
Vol 80 (5) ◽  
pp. 639-646 ◽  
Author(s):  
Saman A. Nasrollahi ◽  
Changiz Taghibiglou ◽  
Ebrahim Azizi ◽  
Effat S. Farboud
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Cell Penetrating Peptides ◽  
Transdermal Drug Delivery System ◽  
Cell Penetrating

Cell-Penetrating Peptides as a Potential Drug Delivery System for Effective Treatment of Diabetes.

2020 ◽  
Vol 26 ◽  
Author(s):  
Mallikarjuna Korivi ◽  
Yue-Wern Huang ◽  
Betty R. Liu
Keyword(s):  
Drug Delivery ◽  
Effective Treatment ◽  
Drug Delivery System ◽  
Delivery System ◽  
Therapeutic Agents ◽  
Cell Penetrating Peptides ◽  
Therapeutic Benefits ◽  
Increased Risk ◽  
Cell Penetrating ◽  
Treatment Of Diabetes

Background/Purpose: Type 2 diabetes (T2D) is characterized by hyperglycemia resulting from the body’s inability to produce and/or use insulin. Patients with T2D often have hyperinsulinemia, dyslipidemia, inflammation, and oxidative stress, which then lead to hypertension, chronic kidney disease, cardiovascular disease, and increased risk of morbidity and mortality (9th leading cause globally). Insulin and related pharmacological therapies are widely used to manage T2D, despite their limitations. Efficient drug delivery systems (DDS) that control drug kinetics may decrease side effects, allow for efficient targeting, and increase the bioavailability of drugs to achieve maximum therapeutic benefits. Thus, development of effective DDS is crucial to beat diabetes. Methods: Here, we introduced a highly bioavailable vector, cell-penetrating peptides (CPPs), as a powerful DDS to overcome limitations of free drug administration. Results: CPPs are short peptides that serve as a potent tool for delivering therapeutic agents across cell membranes. Various cargoes, including proteins, DNA, RNA, liposomes, therapeutic molecules, and nanomaterials, generally retain their bioactivity upon entering cells. The mechanisms of CPPs/cargoes intracellular entry are classified into two parts: endocytic pathways and direct membrane translocation. In this article, we focus on the applications of CPPs/therapeutic agents in the treatment of diabetes. Hypoglycemic drugs with CPPs intervention can enhance therapeutic effectiveness, and CPP-mediated drug delivery can facilitate the actions of insulin. Numerous studies indicate that CPPs can effectively deliver insulin, produce synergistic effects with immunosuppressants for successful pancreatic islet xenotransplantation, prolong pharmacokinetics, and retard diabetic nephropathy. Conclusions: We suggest that CPPs can be a new generation of drug delivery system for effective treatment and management of diabetes and diabetes-associated complications.

The in vivo transformation and pharmacokinetic properties of a liquid crystalline drug delivery system

2017 ◽  
Vol 532 (1) ◽  
pp. 345-351 ◽  
Author(s):  
Andrew Otte ◽  
Yahira M. Báez-Santos ◽  
Ellina A. Mun ◽  
Bong-Kwan Soh ◽  
Young-nam Lee ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Liquid Crystalline ◽  
Pharmacokinetic Properties

Dissolution and Pharmacokinetic Properties of Alkaloids and Flavonoids in a Xiexin Multiple-unit Drug Delivery System

Drug Research ◽  
2013 ◽  
Vol 63 (10) ◽  
pp. 501-509 ◽  
Author(s):  
Y. Xie ◽  
Y. Hu ◽  
M. Shen ◽  
Y. Ma ◽  
J. Zhong ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Pharmacokinetic Properties ◽  
Multiple Unit

scholarly journals Photo-Responsive Polymersomes as Drug Delivery System for Potential Medical Applications

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 5147
Author(s):  
Wanting Hou ◽  
Ruiqi Liu ◽  
Siwei Bi ◽  
Qian He ◽  
Haibo Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Block Copolymers ◽  
Drug Delivery System ◽  
Delivery System ◽  
Raft Polymerization ◽  
Amphiphilic Block Copolymers ◽  
Medical Applications ◽  
Drug Molecules ◽  
Reversible Addition ◽  
Raft Agent

Due to a strong retardation effect of o-nitrobenzyl ester on polymerization, it is still a great challenge to prepare amphiphilic block copolymers for polymersomes with a o-nitrobenzyl ester-based hydrophobic block. Herein, we present one such solution to prepare amphiphilic block copolymers with pure poly (o-nitrobenzyl acrylate) (PNBA) as the hydrophobic block and poly (N,N’-dimethylacrylamide) (PDMA) as the hydrophilic block using bulk reversible addition-fragmentation chain transfer (RAFT) polymerization of o-nitrobenzyl acrylate using a PDMA macro-RAFT agent. The developed amphiphilic block copolymers have a suitable hydrophobic/hydrophilic ratio and can self-assemble into photoresponsive polymersomes for co-loading hydrophobic and hydrophilic cargos into hydrophobic membranes and aqueous compartments of the polymersomes. The polymersomes demonstrate a clear photo-responsive characteristic. Exposure to light irradiation at 365 nm can trigger a photocleavage reaction of o-nitrobenzyl groups, which results in dissociation of the polymersomes with simultaneous co-release of hydrophilic and hydrophobic cargoes on demand. Therefore, these polymersomes have great potential as a smart drug delivery nanocarrier for controllable loading and releasing of hydrophilic and hydrophobic drug molecules. Moreover, taking advantage of the conditional releasing of hydrophilic and hydrophobic drugs, the drug delivery system has potential use in medical applications such as cancer therapy.

Enzyme-triggered delivery of chlorambucil from conjugates based on the cell-penetrating peptide BP16

2015 ◽  
Vol 13 (5) ◽  
pp. 1470-1480 ◽  
Author(s):  
Marta Soler ◽  
Marta González-Bártulos ◽  
Eduard Figueras ◽  
Xavi Ribas ◽  
Miquel Costas ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Cells ◽  
Drug Delivery System ◽  
Delivery System ◽  
Cell Penetrating Peptide ◽  
Cell Penetrating ◽  
Uptake And Release

The combination of the cell-penetrating peptide BP16 with the enzymatic cleavable sequence Gly-Phe-Leu-Gly constitutes a drug delivery system for the effective uptake and release of chlorambucil in cancer cells.

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