Chemical and Physical Enhancers for Transdermal Drug Delivery

Escobar-Chávez, José Juan; Rodríguez-Cruz, Isabel Marlen; Domínguez-Delgado, Clara Luisa

doi:10.5772/33194

Cited by 7 publications

(3 citation statements)

References 181 publications

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“…Efek tarikan dapat dijelaskan bahwa enhancer kimia merubah struktur transpormasi stratum korneum sehingga dapat meningkatkan kelarutan obat ke dalam stratum korneum atau membawa obat berdifusi melewati kulit [8]. [8] Enhancer kimia idealnya memiliki sifat sebagai berikut: tidak toksik, tidak mengiritasi, tidak menimbulkan alergi, bekerja cepat, aktivitasnya dapat diprediksi dan reprodusibel, tidak menimbulkan efek farmakologi (inert), cepat pemulihan, dapat kompatibel dengan obat dan eksipien, serta idelanya tidak berbau dan tidak berwarna [9]. Enhancer kimia dapat diklasifikasikan berdasarkan struktur kimia atau berdasarkan mekanisme aksinya.…”

Section: Enhancer Kimiaunclassified

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Review Artikel: Metode untuk Meningkatkan Absorpsi Obat Transdermal

Annisa¹

2020

J. Islamic Pharm.

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The route of administration of transdermal drugs is preferred because it is easy to use. However, there are limitations associated with the difficulty of drugs penetrating into the skin. This is caused by the presence of the stratum corneum which is the main barrier for drug entry into the skin. Penetration of the drug into the skin can be through the trans-epidermal (transcellular and paracellular) route and the trans-appendegeal route depending on the dosage form. To increase the penetration ability of transdermal drugs, it can use chemical enhancers and physical enhancers. Chemical enhancers can be classified based on chemical structure or based on the mechanism of action. Chemical compounds that have the same functional groups can have different mechanisms of action depending on the physical-chemical nature. Chemical enhancers are categorized based on their chemical structure, including: water, alcohol, amides, esters, alcohol ethers, pyrrolidone, hydrocarbons, sulfides, surfactants, terpenes, phospholipids, vesicles. Whereas physical enhancers in the form of drug delivery use external energy to encourage or physically damage the stratum corneum. Physical enhancer methods such as Iontophoresis,

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Section: Enhancer Kimiaunclassified

“…Voltase yang tinggi akan membentuk jalur/pori sehingga obat dapat melewati stratum korneum. Molekul kecil lipofilik dapat berpartisi ke dalam stratum korneum, tetapi molekul hidrofilik atau molekul bermuatan tidak dapat penetrasi secara signifikan [9].…”

Section: Elektroporasiunclassified

Review Artikel: Metode untuk Meningkatkan Absorpsi Obat Transdermal

Annisa¹

2020

J. Islamic Pharm.

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“…Several techniques such as chemical enhancers, prodrug, iontophoresis, microneedle, electroporation, etc. have been applied to improve the skin permeability of drugs. − Similarly, for the enhancement of intestinal drug permeability, some commonly used methods include nanoemulsions, cyclodextrin-included complexes, spray freeze-drying, use of straight chain fatty acids, and self-microemulsifying drug delivery systems. − In this context, pharmaceutical cocrystallization is an emerging and highly effective technique to improve intestinal permeability as well as transdermal transport of drugs. Cocrystallization is a supramolecular aggregation-based phenomenon of two or more different chemical entities in a crystal lattice through hydrogen bonds and/or noncovalent intermolecular interactions .…”

Section: Introductionmentioning

confidence: 99%

Diffusion and Flux Improvement of Drugs through Complexation

2023

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Improving the solubility and permeability of drugs via cocrystallization is an important theme in crystal engineering with practical applications for the discovery and development of high bioavailability medicines. The past decade has witnessed a surge of publications on pharmaceutical cocrystals/salts to improve the permeability of Biopharmaceutics Classification System (BCS) class IV drugs. In this review article, the reader is introduced to the fundamentals of drug permeability mechanisms and then examples of pharmaceutical cocrystals and salts designed to enhance drug diffusion and permeability are presented, in order to understand the different structural factors that modulate drug flux and transport across a semipermeable membrane. Broadly, two main phenomena can be summarized from the 50 or so examples: (1) The heterosynthons in hydrogen-bonded drug–coformer aggregates survive long enough in the experimental media such that the drug, which is present in high concentration due to supersaturation, exhibits higher flux across the semipermeable membrane. (2) The coformer or cocrystal is able to reduce the transepithelial electrical resistance (TEER) values of lipid monolayers, which impairs their tight junctions, and facilitates drug passage to improve its diffusion/permeability. The medicinal chemistry literature on high permeability drugs is recapitulated with the idea that these principles may be utilized in the de novo design of high permeability coformers for the synthesis of improved-performance pharmaceutical cocrystals. Enhancing drug solubility and permeability without changing its molecular structure in supramolecular complexes of pharmaceutical cocrystals and salts will address the poor bioavailability challenge for a majority of BCS class II and IV drugs.

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