A transdermal review on permeation of drug formulations, modifier compounds and delivery methods

Rai, Vishwas; Ghosh, Indrajit; Bose, Sonali; Silva, S.M.C.; Chandra, Prafulla; Michniak‐Kohn, Bozena

doi:10.1016/s1773-2247(10)50011-x

Cited by 18 publications

(14 citation statements)

References 105 publications

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“…Most permeation enhancers enhance drug uptake through biological membranes by affecting the barrier properties of the membrane itself, either by altering the structure of the cell membrane (passive transcellular route) or by opening of the tight junctions (paracellular route). [230][231][232] For example, chemical enhancers, such as fatty acids, alcohols, amines and amides, permeate into the membrane where they may alter the overall solvent potential of the membrane and disrupt the ordered lipid structure within the membrane barrier thereby lowering the viscosity. These physicochemical changes facilitate drug partition from the exterior into the membrane as well as drug permeation through the membrane barrier.…”

Section: Permeation Enhancersmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes

Loftsson

Brewster

2011

Journal of Pharmacy and Pharmacology

233

126

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Objectives Cyclodextrins are useful solubilizing excipients that have gained currency in the formulator's armamentarium based on their ability to temporarily camouflage undesirable physicochemical properties. In this context cyclodextrins can increase oral bioavailability, stabilize compounds to chemical and enzymatic degradation and can affect permeability through biological membranes under certain circumstances. This latter property is examined herein as a function of the published literature as well as work completed in our laboratories. Key findings Cyclodextrins can increase the uptake of drugs through biological barriers if the limiting barrier component is the unstirred water layer (UWL) that exists between the membrane and bulk water. This means that cyclodextrins are most useful when they interact with lipophiles in systems where such an UWL is present and contributes significantly to the barrier properties of the membrane. Furthermore, these principles are used to direct the optimal formulation of drugs in cyclodextrins. A second related critical success factor in the formulation of cyclodextrin-based drug product is an understanding of the kinetics and thermodynamics of complexation and the need to optimize the cyclodextrin amount and drug-to-cyclodextrin ratios. Drug formulations, especially those targeting compartments associated with limited dissolution (i.e. the eye, subcutaneous space, etc.), should be carefully designed such that the thermodynamic activity of the drug in the formulation is optimal meaning that there is sufficient cyclodextrin to solubilize the drug but not more than that. Increasing the cyclodextrin concentration decreases the formulation 'push' and may reduce the bioavailability of the system. Conclusions A mechanism-based understanding of cyclodextrin complexation is essential for the appropriate formulation of contemporary drug candidates.

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Section: Permeation Enhancersmentioning

confidence: 99%

Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes

Loftsson

Brewster

2011

Journal of Pharmacy and Pharmacology

233

126

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“…A transdermal medication is intended for external use to have localized action near or at the site of application [23]. In comparison to ordinary topical preparations, transdermal formulations are specifically designed to penetrate through the deeper skin layer and to treat the target beneath.…”

Section: Introductionmentioning

confidence: 99%

Electrospun poly(lactic acid) nanofiber mats for controlled transdermal delivery of essential oil from Zingiber cassumunar Roxb

Wongkanya

Teeranachaideekul

Makarasen

et al. 2020

Mater. Res. Express

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A controlled release system of Plai (Zingiber cassumunar Roxb.) oil based on electrospun poly(lactic) acid (PLA) nanofiber mat was successfully developed. The physicochemical properties of the nanofibers loaded with select amounts of oil (15%, 20%, and 30% wt) were characterized using various techniques, including a morphological study using scanning electron microscopy (SEM), structural determination using Fourier transform infrared spectrometry (FTIR) and x-ray diffraction (XRD), as well as thermal properties study using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). The loading content and the entrapment efficiency of Plai oil within the fiber mats were evaluated and were found to be remarkably high, ensuring that PLA was an appropriate material for Plai oil loading. The ability of the nanofiber mats to release (E)-1-(3,4dimethoxyphenyl) butadiene (DMPBD) was also examined and the fiber mats showed controlled release characteristics. As the nanofiber mats have particularly high specific surface area with fully accessible and interconnected pore structures, a liquid medium with active ingredients will not be trapped in blind pores but can be fully released out of the fiber matrix. Furthermore, in vitro skin permeation of the active compound as well as a skin irritation were assessed using reconstructed human epidermis (EpiSkin TM ). It was found that DMPBD could efficiently penetrate through the skin model. Moreover, the nanofiber mats containing Plai oil also showed no skin irritation, indicating them as promising prototypes for medical applications.

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“…[17,18] The drug diffusion test was carried out using male rabbits in which the abdominal skin of rabbits (3.5 kg) was used after completing all the ethical needs including anesthesia with chloroform. The skin was carefully shaved using an electronic clipper, and a full-thickness skin (i.e., epidermis, subcutaneous, and dermis) was excised under esthetic effect.…”

Section: Baclofen Diffusion Study Using Animal Live Skinmentioning

confidence: 99%

Untitled

Ali

2017

AJP

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Aim: The aim of this study is to formulate and evaluate of baclofen transdermal patches using different polymers, penetration enhancers, and plasticizers. A drug with different film forming polymers was subjected to compatibility study. In addition, in-vitro permeation across animal skin for the best formulation was investigated. Materials and Methods: After studying the incompatibility of baclofen and other polymers used, the pure drug baclofen was formulated as transdermal patches composed of different polymers by solvent evaporation method and the formulations were 16. Then, the physicochemical properties of formulated patches were evaluated to determine the best optimum formula to be examined in-vitro release. Results and Discussion: The drug excipient compatibility study revealed no interaction between baclofen and polymers used. All the physicochemical studies of formulated patches were satisfactory except the formulation. The best-chosen formula was F13 that composed of polyvinyl alcohol as film-forming polymer and Carbopol 940 as bioadhesive polymer with propylene glycol as plasticizer and dimethyl sulfoxide as penetration enhancer. Conclusion: Study indicates that baclofen can be formulated as transdermal patches of acceptable appearance and suitable drug release through 24 h.

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A transdermal review on permeation of drug formulations, modifier compounds and delivery methods

Cited by 18 publications

References 105 publications

Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes

Pharmaceutical applications of cyclodextrins: effects on drug permeation through biological membranes

Electrospun poly(lactic acid) nanofiber mats for controlled transdermal delivery of essential oil from Zingiber cassumunar Roxb

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