Transdermal drug delivery by passive diffusion and iontophoresis: A review

Singh, Sanjay; Singh, Jagdish

doi:10.1002/med.2610130504

Cited by 121 publications

(48 citation statements)

References 250 publications

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“…Furthermore, except for sodium salt, all the salts have lower melting points than the parent drug and higher permeability through the skin, which support previous reports, suggesting that a decrease in melting point or conversion of solid state to liquid state improves the permeability of drugs through skin (Singh & Singh, 1993).…”

Section: Determination Of Aqueous Solubilitysupporting

confidence: 89%

Enhanced skin permeation of 6-methoxy-2-naphthylacetic acid by salt formation

et al. 2014

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The aim of this work was to prepare salts of 6-methoxy-2-naphthylacetic acid (6-MNA) to improve its physicochemical properties for percutaneous application. 6-MNA, an active metabolite of non-steroidal anti-inflammatory drug nabumetone has long half life and has the tendency to penetrate well into synovial fluid. The physicochemical properties of 6-MNA salts were investigated by solubility measurements, differential scanning calorimetry (DSC) and infrared (IR). The DSC thermograms and Fourier transform infrared (FT-IR) spectra indicated that 6-MNA formed salts with organic and alkali metal bases. Among the series, salts formed with amine bases (ethanolamine, diethanolamine, triethanolamine and diethylamine) had lower melting points while alkali metal salt (sodium) had higher melting point than 6-MNA. The salts had higher solubilities than 6-MNA as determined in phosphate buffer at pH 5.0 and 7.4. There is no significant difference in partition coefficient (log P) values between salts and 6-MNA at pH 5.0 but, at pH 7.4, the log P values for the salts increased by 4-10 times as compared to 6-MNA. In vitro permeation studies showed that all the salts increased the flux in comparision to 6-MNA, and the ethanolamine salt (1b) was found to be having 7.7 and 9.4 times higher permeability as compared to 6-MNA at pH 5.0 and 7.4, respectively.

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Section: Determination Of Aqueous Solubilitysupporting

confidence: 89%

Enhanced skin permeation of 6-methoxy-2-naphthylacetic acid by salt formation

et al. 2014

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“…In the pharmaceutical, cosmetic and agrochemical industries, predicting the rate of skin permeability is a crucial parameter for transdermal administration of medications and for the risk assessment of chemical products that come into contact with the skin accidentally [52]. The test set compounds showed negative values of skin permeability, i.e, it is not important to be administered for transdermal use, and also not present any risk accordance results described in Table 7.…”

Section: Pharmacokinetic and Toxicological Resultsmentioning

confidence: 99%

A QSAR, Pharmacokinetic and Toxicological Study of New Artemisinin Compounds with Anticancer Activity

et al. 2014

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Abstract:The Density Functional Theory (DFT) method and the 6-31G** basis set were employed to calculate the molecular properties of artemisinin and 20 derivatives with different degrees of cytotoxicity against the human hepatocellular carcinoma HepG2 line. Principal component analysis (PCA) and hierarchical cluster analysis (HCA) were employed to select the most important descriptors related to anticancer activity. The significant molecular descriptors related to the compounds with anticancer activity were the ALOGPS_log, Mor29m, IC5 and GAP energy. The Pearson correlation between OPEN ACCESSMolecules 2014, 19 10671 activity and most important descriptors were used for the regression partial least squares (PLS) and principal component regression (PCR) models built. The regression PLS and PCR were very close, with variation between PLS and PCR of R 2 = ±0.0106, R 2 ajust = ±0.0125, s = ±0.0234, F (4,11) = ±12.7802, Q 2 = ±0.0088, SEV = ±0.0132, PRESS = ±0.4808 and S PRESS = ±0.0057. These models were used to predict the anticancer activity of eight new artemisinin compounds (test set) with unknown activity, and for these new compounds were predicted pharmacokinetic properties: human intestinal absorption (HIA), cellular permeability (P CaCO2 ), cell permeability Maden Darby Canine Kidney (P MDCK ), skin permeability (P Skin ), plasma protein binding (PPB) and penetration of the blood-brain barrier (C Brain/Blood ), and toxicological: mutagenicity and carcinogenicity. The test set showed for two new artemisinin compounds satisfactory results for anticancer activity and pharmacokinetic and toxicological properties. Consequently, further studies need be done to evaluate the different proposals as well as their actions, toxicity, and potential use for treatment of cancers.

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“…Consequently, drug delivery through the skin has been the subject of extensive research [1]. In addition to formulations [2] and chemical enhancers [3], a number of physical methods such as iontophoresis [4,5], electroporation [6,7], and ultrasound (phonophoresis) [8] have been used to facilitate transport of a variety of molecules across the stratum corneum (SC). Photomechanical waves (PW) have been recently shown to facilitate transdermal delivery.…”

Section: Introductionmentioning

confidence: 99%