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Proteins & Peptides Transdermal Delivery System Development

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Transdermal drug delivery is a non-invasive or minimally invasive method that allows a certain amount of drug to penetrate the epidermis of the skin through free diffusion or other means and continuously enter the systemic blood circulation at a controlled rate. As an expert in the development of protein/peptide delivery systems, CD Formulation is committed to assisting our global customers in developing powerful protein/peptide transdermal delivery products through a variety of transdermal enhancement strategies.

Potential Advantages for Transdermal Delivery of Protein/Peptide

One of the most important advantages of the transdermal route is the ability to maintain constant and prolonged release of the drug to achieve optimal blood circulation concentrations. For skin protein/peptide delivery, transdermal delivery has the following potential advantages:

  • Improved bioavailability.
  • Reduced dosing frequency.
  • Reduced adverse reactions caused by medication.
  • Constant plasma levels.
  • Microneedle delivery does not affect the pharmacological activity of the protein/peptide drug.
  • Microneedle delivery does not change the effectiveness of the protein/peptide drug.
  • No side effects.
  • High storage capacity of transdermal microneedle protein/peptide drugs.

Explore Our Proteins & Peptides Transdermal Delivery System Development Services

As one of the global leaders in the development of protein/peptide delivery systems, CD Formulation has the most advanced technology and knowledge in the industry, focusing on combining advanced formulation technology and protein/peptide science to develop powerful transdermal delivery products.

All of our protein/peptide transdermal delivery system development services are performed in GMP-certified laboratories. Our extensive experience in protein/peptide transdermal delivery system development and unique project management approach enables you to achieve rapid success and help you accelerate product launch.

To address the challenge of hydrophilic and large molecular proteins/peptides having difficulty penetrating the stratum corneum barrier during transdermal administration, our scientists deploy a range of single or combined strategies to support the development of protein/peptide transdermal delivery systems.

Fig. 1 Strategies for enhancing proteins/peptide transdermal delivery. Fig. 1 Strategies to enhance the transdermal delivery of protein/peptide. (CD Formulation)

Formulation Strategy

  • Chemical Enhancers
    Chemical penetration enhancers are a good choice to allow proteins/peptides to pass through the skin. Our scientists screen and test different enhancers for their penetration-enhancing effects on your therapeutic proteins/peptides. Commonly used penetration enhancers include D-limonene, azone, lauric acid, glyceryl monooleate, and sodium lauryl sulfate.
  • Transdermal Peptides (Cell-penetrating Peptides, CPP)
    Transdermal mediator peptides are also a type of chemical enhancer. This substance is composed of natural or synthetic polypeptides, which have certain hydrophilicity and lipophilicity and can promote protein/peptide biomolecules to pass through the skin barrier. Transdermal mediator peptides promote drug crossing through various pathways, such as promoting endocytosis of intracellular vesicles, changing the structure of the stratum corneum, and increasing the diffusion rate of drugs in the skin.
  • Nanocarriers
    Our scientists encapsulate protein/peptide drugs in nanocarriers or modify the surface to enhance skin penetration. Nano transdermal delivery carriers that can be developed include nanofibers, nanospheres, nano and microcapsules, polymer vesicles, polymer micelles, and nanogels.

Transdermal Microneedles(MNs) Strategy

Transdermal MNs allow protein/peptide molecules of different sizes to pass through, using the microneedle channel as a channel for these molecules to enter and pass through the skin and reach the blood faster. Depending on your protein/peptide delivery needs, our scientists can develop hollow or solid dissolvable protein transdermal microneedles, as well as degradable and coated or uncoated protein/peptide transdermal microneedles.

Physical Enhancement Strategy

We can employ physical enhancement techniques such as iontophoresis, electroporation, or ultrasound to enhance the transdermal delivery of proteins and peptides.

Combination Strategy

Our scientists use a combination of transdermal enhancement technologies to achieve a synergistic effect in protein/peptide delivery. A typical combination strategy is to combine nanocarrier technology with microneedles, i.e., the internal structure of microneedles contains nano-sized protein/peptide drugs, and the microneedle channels are used to deliver these nano-sized molecules into and through the skin.

Our Expertise for Proteins & Peptides Transdermal Delivery System

Our transdermal delivery expertise and experience allow us to develop a variety of protein/peptide transdermal formulations, including but not limited to protein/peptide transdermal patches, protein/peptide transdermal microneedles, and protein/peptide transdermal gels. We use advanced technology and formulations to ensure that the drug can quickly and effectively cross the skin barrier to achieve the best therapeutic effect.

  • Characterization of therapeutic proteins/peptides.
  • Protein/peptide transdermal enhancement studies.
  • In vitro release and in vitro permeation testing of protein/peptide formulations.
  • Safety evaluation: Conduct safety evaluation of transdermal delivery systems, including evaluation of skin irritation, allergy, etc.
  • Manufacturing process development, including research on packaging material compatibility and evaluation of various sterilization techniques and their effects on products.
  • Quality control testing: Establish a complete quality control system, including strict testing and control of protein/peptide preparation, stability, purity, etc.
  • Analytical method and process transfer.

Capabilities for In Vitro Release Testing(IVRT) & In vitro penetration testing (IVPT)

IVRT and IVPT are two key tests used in transdermal protein/peptide drug development to evaluate the release and permeation of protein/peptide active pharmaceutical ingredients (API).

  • IVRT testing is used to measure the rate and extent of drug release from a patch under simulated physiological conditions, helping to determine the drug release profile of a product and ensure that the drug is released in a consistent and predictable manner.
  • IVPT testing is used to evaluate the permeability of a drug through biological barriers such as the skin or mucous membranes, helping to assess the ability of a drug to penetrate the barrier and reach the target site of action and the distribution of the drug in the skin.

The options for IVRT and IVPT performed by our transdermal experts using the classic static vertical diffusion cell (i.e., Franz cell) include:

Fig. 2 Static vertical diffusion cell. Fig. 2 Static vertical diffusion Franz cells. (Supe S, et al., 2021)

  • Development, validation, and transfer of IVPT analytical methods for protein and peptide transdermal formulations.
  • Optimization and characterization of performance of protein and peptide transdermal formulations.
  • Bioequivalence study of generic and original drugs.
  • Permeation profile and permeation kinetics analysis of protein and peptide transdermal formulations.

Our Solutions for Proteins & Peptides Transdermal Delivery System Development?

  • Extensive expertise and experience in executing protein/peptide transdermal delivery system development.
  • We have a highly skilled formulation science team with decades of experience in developing various protein/peptide transdermal drug delivery systems.
  • Our laboratories are equipped with advanced technology and equipment, and we continuously strive to improve our internal processes using the most advanced technologies and methods.
  • We provide comprehensive analytical testing services to support the development of various protein/peptide transdermal dosage forms, including but not limited to transdermal patches, transdermal gels, and transdermal microneedles.
  • We provide flexible and tailored solutions to meet our customers' specific needs and requirements.
  • Fast and efficient services ensure that our customers' projects are delivered on time.

Publication

Published Data

Technology: Transdermal Peptides/Cell-penetrating Peptides

Journal: Sci Rep.

IF: 4.99

Published: 2022

Results:

The authors evaluated MTD 1067 as cell-penetrating peptides (CPPs) for transdermal delivery of proteins of various sizes, including growth hormone-releasing hexapeptide-6 (GHRP-6), a truncated form of insulin-like growth factor-I (des(1-3)IGF-I), and platelet-derived growth factor BB (PDGF-BB). All MTD 1067-conjugated cargoes exhibited equivalent or enhanced bioactivity compared to the original cargoes. Confocal microscopy image analysis revealed that the levels of MTD-GHRP-6, MTD-des(1-3)IGF-I, and MTD-PDGF-BB detected in the dermis were 4.4-fold, 18.8-fold, and 32.9-fold higher, respectively, compared to the control group without MTD. In addition, the MTD 1067-conjugated cargoes showed no cytotoxicity. This demonstrates the potential of MTD 1067 as a CPP.

Fig. 3 Transdermal delivery of MTD 1067-conjugated peptide and recombinant proteins. Fig. 3 Transdermal delivery of MTD 1067-conjugated peptide and recombinant proteins in artificial skin model. (Shin HJ, et al., 2022)

CD Formulation is always at the forefront of protein/peptide transdermall delivery system development, mastering the most cutting-edge technologies and methods. Please don't hesitate to contact us if you are interested in our services.

References

  1. Peña-Juárez MC, Guadarrama-Escobar OR, Escobar-Chávez JJ. Transdermal Delivery Systems for Biomolecules. J Pharm Innov. 2022;17(2):319-332.
  2. Long L, Zhang J, Yang Z, et al. Transdermal delivery of peptide and protein drugs: Strategies, advantages and disadvantages. Journal of Drug Delivery Science and Technology. 2020, 60: 102007.
  3. Kalluri H, Banga AK. Transdermal delivery of proteins. AAPS PharmSciTech. 2011, 12(1):431-41.
  4. Supe S, Takudage P. Methods for evaluating penetration of drug into the skin: A review. Skin Res Technol. 2021, 27(3):299-308.
  5. Shin HJ, Bak SU, La HN, et al. Efficient transdermal delivery of functional protein cargoes by a hydrophobic peptide MTD 1067. Sci Rep. 2022,12(1):10853.
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