Transdermal Delivery of biopharmaceuticals: Dream or reality?

Katikaneni, Sahitya

doi:10.4155/tde.15.60

Cited by 13 publications

(13 citation statements)

References 25 publications

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“…It is also a complex and efficient barrier to their penetration in the body. 4,5 It is made of three layers: the epidermis, the dermis, and the hypodermis. 1,2 The skin acts as a barrier, and this function is largely attributed to the outmost layer, the stratum corneum (SC), which is made of overlapping layers of nonviable keratocytes called corneocytes.…”

Section: ■ Introductionmentioning

confidence: 99%

High-Sensitivity Permeation Analysis of Ultrasmall Nanoparticles Across the Skin by Positron Emission Tomography

et al. 2021

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Ultrasmall nanoparticles (US-NPs; <20 nm in hydrodynamic size) are now included in a variety of pharmacological and cosmetic products, and new technologies are needed to detect at high sensitivity the passage of small doses of these products across biological barriers such as the skin. In this work, a diffusion cell adapted to positron emission tomography (PET), a highly sensitive imaging technology, was developed to measure the passage of gold NPs (AuNPs) in skin samples in continuous mode. US-AuNPs (3.2 nm diam.; TEM) were functionalized with deferoxamine (DFO) and radiolabeled with 89Zr(IV) (half-life: 3.3 days, matching the timeline of diffusion tests). The physicochemical properties of the functionalized US-AuNPs (US-AuNPs-PEG-DFO) were characterized by FTIR (DFO grafting; hydroxamate peaks: 1629.0 cm–1, 1569.0 cm–1), XPS (presence of the OC–N C 1s peak of DFO at 287.49 eV), and TGA (organic mass fraction). The passage of US-AuNPs-PEG-DFO-89Zr(IV) in skin samples was measured by PET, and the diffusion parameters were extracted thereby. The signals of radioactive US-AuNPs-PEG-DFO-89Zr(IV) leaving the donor compartment, passing through the skin, and entering the acceptor compartment were detected in continuous at concentrations as low as 2.2 nM of Au. The high-sensitivity acquisitions performed in continuous allowed for the first time to extract the lag time to the start of permeation, the lag time to start of the steady state, the diffusion coefficients, and the influx data for AuNPs permeating into the skin. PET could represent a highly valuable tool for the development of nanoparticle-containing topical formulations of drugs and cosmetics.

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Section: ■ Introductionmentioning

confidence: 99%

High-Sensitivity Permeation Analysis of Ultrasmall Nanoparticles Across the Skin by Positron Emission Tomography

et al. 2021

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“…After that, a sum total of 91 protein based drugs manufactured by recombinant technology have been approved by the FDA [5]. Specificity attributed by the complex structural orientation of proteins and potency has been the cornerstone of protein based therapeutics as compared to small molecule drugs [1,6]. However, stability related matters, complexity of their nature lend the proteins difficult for delivery.…”

Section: Introduction: Transdermal Route and Protein Deliverymentioning

confidence: 99%

“…However, limitations like GI degradation, low bioavailability and local irritation persist [7]. In such scenario, skin could be the potential alternative for administration of protein drugs across the skin as it bypasses the first pass metabolism, offers prolonged release of drug and exhibits minimal proteolytic activity compared to other routes [6]. Figure 1 shows physical techniques of transdermal drug delivery.…”

Section: Introduction: Transdermal Route and Protein Deliverymentioning

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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“…The drug molecules are then transported to the target site, which could be relatively remote from the site of administration, to produce therapeutic action. 3 NFDP is a calcium channel blocker with vasodilatory properties due to the enhancement of endothelial nitric oxide release, which causes relaxation of vascular smooth muscle. It is used in the treatment of hypertension by decreasing heart rate and myocardial contractility.…”

Section: Introductionmentioning

confidence: 99%

Preparation of Transdermal Films of Nifedipine: Ex-vivo and In-vitro Studies

Venkateswarlu¹,

Babu²,

Triveni³

et al. 2017

PHME

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Objective: The aim of present study was to prepare and evaluate the transdermal films (TFs) of Nifedipine (NFDP). Methods: The TFs were prepared by solvent evaporation technique and twelve formulations of NFDPTFs were prepared by taking HPMC E15 and Eudragit L100 in different ratios. Polyethylene glycol (15%) and Dimethyl sulfoxide (DMSO) were incorporated as plasticizer and permeation enhancer respectively. DMSO was incorporated in the formulations F7-F12 but it was absent in F1-F6. Results: The prepared TFs were evaluated for weight variation, thickness, folding endurance, drug content, moisture absorption, moisture content determination, mechanical properties and ex-vivo permeation. Mechanical properties revealed that the formulations F4 and F10 were found to be strong enough but not brittle. Hence, the formulations F4 and F10 were selected for ex-vivo studies. The formulations F4 and F10 showed maximum drug permeation within 24 h and formulation with permeation enhancer showed highest drug permeation than formulation without permeation enhancer. Conclusion: It could be concluded that the formulation with permeation enhancer (F10) showed highest permeability through the rat skin than formulation without permeation enhancer.

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Transdermal Delivery of biopharmaceuticals: Dream or reality?

Cited by 13 publications

References 25 publications

High-Sensitivity Permeation Analysis of Ultrasmall Nanoparticles Across the Skin by Positron Emission Tomography

High-Sensitivity Permeation Analysis of Ultrasmall Nanoparticles Across the Skin by Positron Emission Tomography

Passive delivery of protein drugs through transdermal route

Preparation of Transdermal Films of Nifedipine: Ex-vivo and In-vitro Studies

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