Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery

Pawar, Vijay; Thosani, Rushabh; Kanhed, Ashish M.; Giridhar, Rajani; Yadav, Mange Ram

doi:10.1208/s12249-014-0240-6

Cited by 3 publications

(2 citation statements)

References 22 publications

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“…Rat dorsal skin was used in Franz diffusion cells. The 4-ethylpiperazinyl-1-propyl ester prodrug 31 showed a 10-fold higher flux in permeating the skin compared to the parent 28 (16.10 vs. 1.44 nmol/cm 2 /h) [72]. Thus, enhancement of percutaneous absorption was achieved in this study by using the prodrug strategy.…”

Section: The Impact Of Prodrug Strategy On the Percutaneous Absorpmentioning

confidence: 91%

Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs

N’Da

2014

Molecules

127

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Abstract:The transdermal application of drugs has attracted increasing interest over the last decade or so, due to the advantages it offers, compared to other delivery methods. The development of an efficient means of transdermal delivery can increase drug concentrations, while reducing their systemic distribution, thereby avoiding certain limitations of oral administration. The efficient barrier function of the skin, however, limits the use of most drugs as transdermal agents. This limitation has led to the development of various strategies to enhance drug-skin permeation, including the use of penetration enhancers. This method unfortunately has certain proven disadvantages, such as the increased absorption of unwanted components, besides the drug, which may induce skin damage and irritancy. The prodrug approach to increase the skin's permeability to drugs represents a very promising alternative to penetration enhancers. The concept involves the chemical modification of a drug into a bioreversible entity that changes both its pharmaceutical and pharmacokinetic characteristics to enhance its delivery through the skin. In this review; we report on the in vitro attempts and successes over the last decade by using the prodrug strategy for the percutaneous delivery of pharmacological molecules.

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Section: The Impact Of Prodrug Strategy On the Percutaneous Absorpmentioning

confidence: 91%

Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs

N’Da

2014

Molecules

127

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“…The authors designed piperazine derivatives attached by an ester linkage to enhance the solubility of these compounds. They identified a compound 22 that proved to be water soluble and 11.2-fold more permeable through the skin than 6-MNA at pH 7.4 (Figure 10) [45].…”

Section: Ester Prodrugsmentioning

confidence: 99%

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

et al. 2015

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Prodrug design is a widely known molecular modification strategy that aims to optimize the physicochemical and pharmacological properties of drugs to improve their solubility and pharmacokinetic features and decrease their toxicity. A lack of solubility is one of the main obstacles to drug development. This review aims to describe recent advances in the improvement of solubility via the prodrug approach. The main chemical carriers and examples of successful strategies will be discussed, highlighting the advances of this field in the last ten years.

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Microemulsion and bovine serum albumin nanoparticles as a novel hybrid nanocarrier system for efficient multifunctional drug delivery

Gharbavi

Danafar

Sharafi

2020

J Biomedical Materials Res

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The present study aims to: (a) design the versatile microemulsions (MEs) system for drug delivery; (b) use the bovine serum albumin nanoparticles for MEs system development; (c) characterize the physicochemical properties, cytotoxicity, and biocompatibility of the modified MEs (MMEs) system; (d) load of paclitaxel (PTX) and folate conjugate of MEs system; and (e) assess the potential of anticancer activity of MEs system. The physicochemical possessions, in vitro and in vivo cytotoxicity, and stability of MMEs system were characterized. The results of our study show that the MEs system was stable, having narrow particle size distribution, nontoxic, biocompatible, and not active for leukocyte proliferation. So it can be concluded that the MMEs system as a promising candidate for a targeted multifunctional drug delivery system (PTX and folate) that is called a smart MEs system.

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Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery

Cited by 3 publications

References 22 publications

Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs

Prodrug Strategies for Enhancing the Percutaneous Absorption of Drugs

The Prodrug Approach: A Successful Tool for Improving Drug Solubility

Microemulsion and bovine serum albumin nanoparticles as a novel hybrid nanocarrier system for efficient multifunctional drug delivery

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