Physical and chemical penetration enhancers in transdermal drug delivery system

Mathur, Vineet; Satrawala, Yamini; Rajput, Mithun Singh

doi:10.4103/0973-8398.72115

Cited by 83 publications

(52 citation statements)

References 113 publications

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“…All of these methods have respective weaknesses, for instance, the complexity design of prodrugs, irritation or toxicity of chemical enhancers, pain and damage of tissue caused by iontophoresis or noncavitational ultrasound and complex device design of electroporation, etc. [3][4][5][6] Pharmaceutical cocrystals can be defined as a stoichiometric multiple component supramolecular structure combined by an active pharmaceutical ingredient (API) and one or more unique cocrystal formers with non-covalent bonds. 7 Formation of pharmaceutical cocrystals can dramatically ameliorate the physicochemical properties of the API without any disruption of covalent bonds, including melting point, solubility, dissolution rate, stability 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 4 and mechanical behavior, etc.…”

Section: Introductionmentioning

confidence: 99%

Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

Dai

Chen

et al. 2016

Crystal Growth & Design

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Pharmaceutical cocrystallization is proposed as a new method to enhance membrane permeability of a BCS class III model drug, 5-fluorouracil (5FU). Three cocrystals of 5FU, 5FU/3-hydroxybenzoic acid (1), 5FU/4-aminobenzoic acid (2) and 5FU/cinnamic acid (3), were successfully synthesized by a slurry method or a liquid-assisted grinding process. Spectroscopic methods, thermal analysis, and X-ray diffraction were used to characterize these new forms. The permeability was studied using a Franz diffusion cell and silicone membrane. All of the cocrystals showed improved membrane permeability compared to free 5FU. The cumulative amount per unit area of permeated 5FU in the first ten hours for 1-3 were increased by 41%, 70% and 83%, and the steady penetrate rate of 1-3 were increased by 38%, 66% and 79% respectively, as compared to pure drug.Structure-permeability correlation study finds a link between intermolecular interactions and molecular packing in cocrystals and their permeability behavior and has important implications for use of cocrystallization approach to improve drugs' permeability in pharmaceutical field.

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Section: Introductionmentioning

confidence: 99%

Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

Dai

Chen

et al. 2016

Crystal Growth & Design

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“…Therefore, to deliver the therapeutic agents through skin, the SC barrier has to be breach. In recent years, extensive experiments have been carried out to breach the skin barrier56. On the basis of applications, these experiments have been classified in two categories, namely, passive and active methods.…”

mentioning

confidence: 99%

“…On the basis of applications, these experiments have been classified in two categories, namely, passive and active methods. Chemical penetration enhancers and liposomes (passive method) interact with the skin constituents and change the morphology of skin at molecular scale5. Active methods such as electroporation, iontophoresis, sonophoresis and thermophoresis use external energy source (electric current, ionic flux and so on) to create the temporary nano-pores in the SC that lead to the permeation of molecules through skin6.…”

mentioning

confidence: 99%

Effect of Size and Surface Charge of Gold Nanoparticles on their Skin Permeability: A Molecular Dynamics Study

Gupta

Rai

2017

Sci Rep

176

138

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Molecular level understanding of permeation of nanoparticles through human skin establishes the basis for development of novel transdermal drug delivery systems and design and formulation of cosmetics. Recent experiments suggest that surface coated nano-sized gold nanoparticles (AuNPs) can penetrate the rat and human skin. However, the mechanisms by which these AuNPs penetrate are not well understood. In this study, we have carried out coarse grained molecular dynamics simulations to explore the permeation of dodecanethiol coated neutral hydrophobic AuNPs of different sizes (2–5 nm) and surface charges (cationic and anionic) through the model skin lipid membrane. The results indicate that the neutral hydrophobic AuNPs disrupted the bilayer and entered in it with in ~200 ns, while charged AuNPs were adsorbed on the bilayer headgroup. The permeation free energy calculation revealed that at the head group of the bilayer, a very small barrier existed for neutral hydrophobic AuNP while a free energy minimum was observed for charged AuNPs. The permeability was maximum for neutral 2 nm gold nanoparticle (AuNP) and minimum for 3 nm cationic AuNP. The obtained results are aligned with recent experimental findings. This study would be helpful in designing customized nanoparticles for cosmetic and transdermal drug delivery application.

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“…Probably this process minimizes the contact area between the hydrophilic and lipophilic lipid domains [10]. Those data suggest that water can react with proteins and lipids, which is compatible with the general construction of the skin [12].…”

Section: Skin-protective Layermentioning

confidence: 56%

Structure and Mechanical Properties of Soft Tissues during Selected Pathological Processes

Kmiecik¹,

Skotny²,

Detyna³

2017

Gen Med (Los Angeles)

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Pathological process often modifies the structure of the soft tissue and can lead changes of mechanical properties. The regularity of this relationship has already been used in the elastography and currently it is applied in medical diagnostic. Tissue stiffness can be identified by a quick measurement but more accurate details can be obtained only by biopsy. Studies, presented in a scientific literature, focus only on pathological stiffness or consider only changes in biochemical structure. These researches revealed two very important components of those modifications -elastin and collagen. Soft tissues are multicomponent, inhomogeneous and anisotropic structures. Their functionality depends on complicated processes on molecular level. Probably the individual components of the tissue can effect on each other. They may promote creation of processes, which can participate in modifications of elasticity. For this reason, it is very important to relate changes on the structural level with mechanical properties. This information can be very helpful in diagnosis and treatment of soft tissue disease.

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Physical and chemical penetration enhancers in transdermal drug delivery system

Cited by 83 publications

References 113 publications

Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

Improving the Membrane Permeability of 5-Fluorouracil via Cocrystallization

Effect of Size and Surface Charge of Gold Nanoparticles on their Skin Permeability: A Molecular Dynamics Study

Structure and Mechanical Properties of Soft Tissues during Selected Pathological Processes

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