Peptides as Skin Penetration Enhancers for Low Molecular Weight Drugs and Macromolecules

Kumar, Sunny; Narishetty, Sunil T.; Tummala, Hemachand

doi:10.1007/978-3-662-47039-8_21

Cited by 9 publications

(8 citation statements)

References 82 publications

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“…SPPs can penetrate skin through the lipid bilayers, and/or through corneocytes, and/or though hair follicles. [165] Peptides which can break down skin or inhibit repair of the SC also act as skin permeation enhancers (See section 3.3.3.2).…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

“…[165] Polyarginine (specifically, with 7 arginine amino acids, i.e. R7), one of the most studied CPPs, can penetrate the SC and reach the dermis of mouse skin.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

“…[165] This property led to their application as permeation enhancers for skin. For example, magainin, a 23-amino acid peptide (Figure 6), is believed to form angstrom-scale pores in the lipid bilayers of the SC.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

“…For example, magainin, a 23-amino acid peptide (Figure 6), is believed to form angstrom-scale pores in the lipid bilayers of the SC. [165] A simple mixture of magainin and the small molecule CPE N-lauroylsarcosine achieved 35- to 92-fold increase in the delivery rate of fluorescein across human epidermis in vitro. [169–170] …”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

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Getting Drugs Across Biological Barriers

et al. 2017

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The delivery of drugs to a target site frequently involves crossing biological barriers. The degree and nature of the impediment to flux, as well as the potential approaches to overcoming it, depend on the tissue, the drug, and numerous other factors. Here we present an overview of approaches that have been taken to crossing biological barriers, with special attention to transdermal drug delivery. Technology and knowledge pertaining to addressing these issues in a variety of organs could have a significant clinical impact.

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Section: Transdermal Drug Deliverymentioning

confidence: 99%

“…[165] Polyarginine (specifically, with 7 arginine amino acids, i.e. R7), one of the most studied CPPs, can penetrate the SC and reach the dermis of mouse skin.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

Section: Transdermal Drug Deliverymentioning

confidence: 99%

Section: Transdermal Drug Deliverymentioning

confidence: 99%

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Getting Drugs Across Biological Barriers

et al. 2017

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“…Skin penetrating peptides. Small peptides (1000-1500 Da) were introduced a decade ago, labelled as skin penetrating peptides (SPPs) as a safer alternative for improved transport of therapeutic molecules both small and large in nature across the skin [54]. Hsu and Mitragotri extensively used this technique and provided the first evidence that SPPs selected by phage display are able to enhance the penetration of macromolecules through human skin and favour the partition of nanocarrier within the epidermis [55].…”

Section: Fatty Acidsmentioning

confidence: 99%

Passive delivery of protein drugs through transdermal route

Chaulagain

Jain

Tiwari

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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Skin is the largest external organ in the human body but its use for therapeutic purposes has been minimal. Stratum corneum residing on the uppermost layer of the skin provides a tough barrier to transport the drugs across the skin. Very small group of drugs sharing Lipinski properties, i.e. drugs having molecular weight not larger than 500 Da, having high lipophilicity and optimum polarity are fortunate enough to be used on skin therapeutics. But, at a time where modern therapeutics is slowly shifting from use of small molecular drugs towards the use of macromolecular therapeutic agents such as peptides, proteins and nucleotides in origin, skin therapeutics need to be evolved accordingly to cater the delivery of these agents. Physical technologies like iontophoresis, laser ablation, micro-needles and ultrasound, etc. have been introduced to enhance skin permeability. But their success is limited due to their complex working mechanisms and involvement of certain irreversible skin damage in some or other way. This review therefore explores the delivery strategies for transport of mainly peptide and protein drugs that do not involve any injuries (non-invasive) to the skin termed as passive delivery techniques. Chemical enhancers, nanocarriers, certain biological peptides and miscellaneous approaches like prodrugs are also thoroughly reviewed for their applications in protein delivery.

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Cell penetrating peptides: Highlighting points in cancer therapy

Asrorov

Wang

Zhang

et al. 2023

Drug Development Research

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Cell‐penetrating peptides (CPPs), first identified in HIV a few decades ago, deserved great attention in the last two decades; especially to support the penetration of anticancer drug means. In the drug delivery discipline, they have been involved in various approaches from mixing with hydrophobic drugs to the use of genetically conjugated proteins. The early classification as cationic and amphipathic CPPs has been extended to a few more classes such as hydrophobic and cyclic CPPs so far. Developing potential sequences utilized almost all methods of modern science: choosing high‐efficiency peptides from natural protein sequences, sequence‐based comparison, amino acid substitution, obtaining chemical and/or genetic conjugations, in silico approaches, in vitro analysis, animal experiments, etc. The bottleneck effect in this discipline reveals the complications that modern science faces in drug delivery research. Most CPP‐based drug delivery systems (DDSs) efficiently inhibited tumor volume and weight in mice, but only in rare cases reduced their levels and continued further processes. The integration of chemical synthesis into the development of CPPs made a significant contribution and even reached the clinical stage as a diagnostic tool. But constrained efforts still face serious problems in overcoming biobarriers to reach further achievements. In this work, we reviewed the roles of CPPs in anticancer drug delivery, focusing on their amino acid composition and sequences. As the most suitable point, we relied on significant changes in tumor volume in mice resulting from CPPs. We provide a review of individual CPPs and/or their derivatives in a separate subsection.

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Peptides as Skin Penetration Enhancers for Low Molecular Weight Drugs and Macromolecules

Cited by 9 publications

References 82 publications

Getting Drugs Across Biological Barriers

Getting Drugs Across Biological Barriers

Passive delivery of protein drugs through transdermal route

Cell penetrating peptides: Highlighting points in cancer therapy

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