Ethanol and Other Alcohols: Old Enhancers, Alternative Perspectives

Heard, Charles Martin

doi:10.1007/978-3-662-47039-8_10

Cited by 5 publications

(3 citation statements)

References 67 publications

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“…Increase in EtOH content to 20% reduced this effect to 1.2-fold. A positive influence of ethanol on the passage of UMF across the membrane is to be expected, since this solvent is known as a penetration enhancer [ 59 ]. At the next step we analyzed the combined impact of F-127 and ethanol on permeability.…”

Section: Resultsmentioning

confidence: 99%

Revisiting the Solubility–Permeability Relationship with Hydrophobic Drug Umifenovir in Pluronic Solutions: Impact of pH and Co-Solvent

2023

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This study describes the influence of pluronic F-127 (F-127) and ethanol (EtOH) on the solubility of umifenovir (UMF) in buffer solutions of pH 2.0 and pH 7.4, and its permeability through cellulose membranes. A 44.4-fold greater UMF solubility in acidic medium as compared to an alkaline one was estimated at 310.15 K. The concentration of UMF in the saturated solution was enhanced by the interaction with F-127 micelles. The combined positive effect of EtOH and F-127 on the solubility was estimated. The aggregation number of F-127 micelles in the presence of 10% and 20% ethanol appeared to be reduced by 2.1-fold and 4.1-fold, respectively, as compared to buffer pH 7.4. The presence of ethanol in buffer pH 7.4 solution provided better solvent conditions but inhibited the formation of F-127 micelles. The impact of UMF on the aggregation number of F-127 was not pronounced and was expressed only by a slight increase of 1 and 3 units in 10% and 20% EtOH, respectively. According to the values of zeta potential, addition of EtOH reduced the stability of the system. The permeation of UMF in buffer pH 7.4 measured through the cellulose membrane MWCO 12–14 kDa was increased 1.4-fold by 10% EtOH. An increase in EtOH content to 20% reduced this effect to 1.2-fold. Decreasing effect of 1.5% F-127 on the permeability was inhibited by using 10% EtOH. The solution containing 1.5% F-127 and 10% EtOH was shown to be an advantageous system for UMF in view of the solubility–permeability balance. The authors suppose the findings of the study to be useful for the design of pharmaceutical formulations based on UMF antiviral drugs.

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Section: Resultsmentioning

confidence: 99%

Revisiting the Solubility–Permeability Relationship with Hydrophobic Drug Umifenovir in Pluronic Solutions: Impact of pH and Co-Solvent

2023

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“…16 Etanol ve propilen glikol gibi çözücüler yalnızca penetrasyon artırıcılar olarak değil, aynı zamanda lipofilik ilaçların çözünürlüğünü artırmak için kosolvan olarak da kullanılmaktadır. 24 Yağ alkolleri ise deri bariyerindeki lipidlerin düzenli yapısını bozarak, ilaç penetrasyonunun artmasını sağlarlar. Penetrasyon artışı, alkil zincirlerinin akışkanlığının artmasına neden olan polar baş grup bölgesi ile yağ alkollerinin etkileşimlerinin bir sonucudur.…”

Section: Ki̇myasal Penetrasyon Artiricilarunclassified

Strategies to Enhance Drug Pass in Transdermal and Dermal Therapeutic Systems: Traditional Review

ÖZCAN,

İLBASMIŞ TAMER

2023

J Lit Pharm Sci

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ÖZET Transdermal ve dermal terapötik sistemlerin diğer ilaç uygulama yollarına göre birçok avantajı bulunmaktadır. Transdermal yol, ilaçların oral yoldan verildiğinde ilk geçiş etkisi gibi mide-bağırsak sisteminde ortaya çıkabilecek sakıncaları önleyebilir, böylece ilaçların biyoyararlanımı artırır. Subkütan enjeksiyona göre daha düşük enfeksiyon riski ve maliyeti vardır. Hasta uyuncu daha yüksektir. Dermal uygulama ise ağrı ve sistemik yan etkileri en aza indirmesi ve kullanım kolaylığı gibi avantajlara sahiptir. Deriden ilaç geçişi hücre içi, hücreler arası, transapendageal ve gözenek yolu ile difüzyonla gerçekleşmektedir. Transdermal ve dermal sistemlerde karşılaşılan en büyük zorluklardan biri, ilaçların deriden geçişlerinin yeterli düzeyde olmamasıdır. Epidermisin en üst katmanı olan stratum korneum (SK), ilaç geçişine karşı engel özelliği göstermektedir. SK'nin hücre dışı lipid ile zenginleştirilmiş matrisi hidrofilik ilaçların geçişini sınırlamakta, lipofilik ilaçların ise birikip yavaşça salınmasına sebep olabilmektedir. Bu durum aktif bileşenlerin biyoyararlanımını düşürmektedir. İlaç taşıyıcı sistemlerin sağladığı avantajlardan faydalanarak, SK'nin engel işlevini aşmak için çeşitli aktif ve pasif yöntemler geniş çapta incelenmiştir. Bu derleme makalede de transdermal ve dermal terapötik sistemlerde ilaç geçişini artırma yöntemleri incelenmiştir. Birinci nesil transdermal ve dermal ilaç taşıyıcı sistemlerde ilaç geçişi çok sınırlıdır. Esas olarak ikinci nesil yöntemlerde ilaç geçişinin artırılması hedeflenmektedir. Bu kapsamda; ilaç-ilaç etkileşimi, SK modifikasyonu, ilaç taşıyıcı sistemler, enerji odaklı sistemler ve SK'nin atlatılması yöntemlerini içermektedir. İkincil nesildeki yöntemlerin birleştirilmesi ise üçüncü nesli oluşturmaktadır. Bu tür yenilikçi yaklaşımlar uygulanan ilaçları doz, maliyet ve terapötik etkinlik açısından daha avantajlı hâle getirebilir. Bu makale kapsamında özellikle ikinci nesil başlığı altında yer alan yöntemler özetlenerek, incelenmiştir. Anah tar Ke li me ler: Kutanöz uygulama; deri emilimi; iyontoforez; elektroporasyon; ilaç taşıyıcı sistem ABS TRACT Transdermal, dermal systems therapeutic systems have many advantages over other drug delivery routes. Transdermal route can prevent problems that may occur in gastrointestinal system such as first pass effect when the drugs are administered orally, increase bioavailability of drugs. It has lower infection risk, cost compared to subcutaneous injection. Patient compliance is higher. Dermal application has advantages such as minimizing pain, systemic side effects, ease of use. Drug passage through skin occurs by diffusion through intracellular, intercellular, transappendageal, pore routes. One of the biggest difficulties encountered in transdermal, dermal systems is insufficient penetration of drugs through skin. Stratum corneum (SC), uppermost layer of the epidermis, acts as barrier against drug penetration. Extracellular lipid-enriched matrix of SC restricts passage of hydrophilic drugs, causing accumulation, slow release of ...

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“…However, there are several parameters that can be considered when attempting to categorize them. Classifications based on their (a) origin, natural [ 39 , 40 , 41 , 42 , 43 ], synthetic [ 44 , 45 , 46 , 47 , 48 ], or semi-synthetic [ 44 , 49 ], and on their (b) chemical structure, alcohols [ 50 , 51 , 52 , 53 ], fatty acids [ 51 , 54 ], surfactants [ 48 , 55 ], esters [ 46 , 51 , 56 , 57 , 58 , 59 , 60 , 61 , 62 ], amides [ 45 , 62 ], and sulfoxides [ 63 , 64 ] are the most common.…”

Section: Chemical Penetration Enhancers (Cpes)mentioning

confidence: 99%

Current Status of Amino Acid-Based Permeation Enhancers in Transdermal Drug Delivery

et al. 2021

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Transdermal drug delivery (TDD) presents many advantages compared to other conventional routes of drug administration, yet its full potential has not been achieved. The administration of drugs through the skin is hampered by the natural barrier properties of the skin, which results in poor permeation of most drugs. Several methods have been developed to overcome this limitation. One of the approaches to increase drug permeation and thus to enable TDD for a wider range of drugs consists in the use of chemical permeation enhancers (CPEs), compounds that interact with skin to ultimately increase drug flux. Amino acid derivatives show great potential as permeation enhancers, as they exhibit high biodegradability and low toxicity. Here we present an overview of amino acid derivatives investigated so far as CPEs for the delivery of hydrophilic and lipophilic drugs across the skin, focusing on the structural features which promote their enhancement capacity.

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Ethanol and Other Alcohols: Old Enhancers, Alternative Perspectives

Cited by 5 publications

References 67 publications

Revisiting the Solubility–Permeability Relationship with Hydrophobic Drug Umifenovir in Pluronic Solutions: Impact of pH and Co-Solvent

Revisiting the Solubility–Permeability Relationship with Hydrophobic Drug Umifenovir in Pluronic Solutions: Impact of pH and Co-Solvent

Strategies to Enhance Drug Pass in Transdermal and Dermal Therapeutic Systems: Traditional Review

Current Status of Amino Acid-Based Permeation Enhancers in Transdermal Drug Delivery

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