Nsaid'ların (non-steroidal anti-inflammatory drug) topikal uygulamaları için yeni jel formulasyonlarının hazırlanması: Kontrollü ilaç salım potansiyellerinin araştırılması
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Tarih
2016
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info:eu-repo/semantics/embargoedAccess
Özet
Amid bağlarıyla iki L-Lizin amino asidinin N6 amino gruplarından oksalil amid linki ile birbirine bağlanmış olan yeni gemini L-Lizin bazlı organojelatörleri, basit ve etkili bir şekilde sentezlenmiş ve organik sıvılardaki jelleşme yetenekleri ve termal kararlılıkları incelenmiştir. Lizinin N? -amino grubunda farklı zincir uzunluklu alkanoil gruplarına sahip (4-6: N? -Alkanoil = lauroil, miristoil, palmitoil), Bis(N? -Alkanoil-N? -L-Lizil-Etil Ester) okzalil amit türevleri, farmasötik organik sıvılar için yeni düşük mol kütleli organo jelatörler (LMWGs) ilaç depo sistemleri olarak geliştirmek üzere incelenmiştir. Steroidal olmayan ilaç molekülü Naproxen örneğinde yeni dermal ve topikal ilaç uygulama aracı olarak açıklanmıştır. Kozmetik endüstrisinde kullanılan farklı zincir uzunluğuna sahip yağ asitlerinin etil ve izopropil esterleri (FAE’ler), likit parafin, 1,2-propandiol, 1-dekanol gibi biyouyumlu organik sıvılar olarak seçilmiştir. Naproksen (Npx) model ilaç olarak, supramoleküler organojel içine hapsedilmiştir. Supramolecular organo jellerden Npx moleküllerinin salım davranışı, UV-vis spektroskopisi kullanılarak incelenmiştir. Npx moleküllerinin salım davranışına, organo jelatorün ve ilacın konsantrasyonunun, alıcı ortamın pH’sının ve çözücünün doğasının (faklı yağ asidi esterleri, Likit Parafin, 1,2-Propandiol, 1-Dekanol) etkisi, statik koşullar altında incelenmiştir. Sonuçlar, supramoleküler organojel içinden Npx’in salım hızının, organojelatör konsantrasyonunun artışı ile etkili bir şekilde yavaşlatılmış olduğunu göstermiştir. Ayrıca Npx’in miktarı arttıkça salınan Npx miktarı da artmaktadır. Fakat salım hızı değişmemektedir. Ayrıca Naproksenin değişik pH’a tamponlanmış alıcı ortam içine salım davranışının farklı olduğu bulundu. Salım kinetiğinin incelenmesi, Npx salımı davranışının Higuchi denklemine ve Fickian modelindeki difüzyon kontrollü mekanizma ile uyumlu olduğu gösterilmiştir. Bu gözlemler; bis(N2 -alkanoil-N6 -L-lizil-etil ester) okzalil amid jellerinin, non-steroidal ilaç moleküllerinin taşınmasında dağıtım aracı olarak ve aynı zamanda bu tür sistemlerin salım profillerinin, doğru jelatör-çözücü kombinasyonunun seçimi ile çok ince bir şekilde ayarlanabileceği gösterilmiştir. Anahtar Kelimeler: Organojel, Organojelatör, İlaç Salım, Naproksen, L-Lizin, SEM, NSAID’s.
Novel gemini organogelators based on L-lysine, in which two L-lysine amino acides are linked by oxalyl amide from it’s N6 amino groups through the amide bond, have been simply and effectively synthesized, and their organogelation abilities and thermal stabilities have been investigated. Bis(N2 -Alkanoyl-N6 -L-Lysyl-Ethyl Ester) Oxalyl Amides derivatives with different chain lenght alkanoyl groups at N2-Lysine moiety (4-6: N2 -Alkanoyl=lauroyl, miristoyl, palmitoyl), as a novel LMWGs for pharmaceutical organic fluids have been explored to develop drug depot systems and illustrated for novel dermal and topical drug delivery vehicle for nonsteroidal drug molecule Naproxene. FAE’s (Faty acid ethyl and isopropyl esters) which have different chain length, liquid paraffin, 1,2-propanediol, 1-decanol have been chosen as a biocompatible organic fluids which are used in cosmetic industry. Naproxene(Npx), acting as a model drug, was entrapped in the supramolecular organogels. The release behavior of Npx molecules in the supramolecular organogels was investigated by using UV–vis spectroscopy. The influence of concentration of the organogelator and drug, pH values of the accepting media, and nature of solvent (different FAE’s, Liquid Paraffin, 1,2-Propanediol, 1-Decanol ) on the release behavior of Npx was investigated under static conditions. The results indicated that the release rate of Npx in the supramolecular organogels was effectively retarded with an increase of the organogelator concentration. Also, the release amount of Npx increased with increasing of the Npx content but this didn’t the change release rate of Npx by increasing of it’s amount. Furthermore, the release behavior of Npx was found to be different at various pH values in buffers as accepting media. The study of the release kinetics indicated that the release behavior of Npx was in accord with the Higuchi equation and the diffusion-controlled mechanism involved in the Fickian model. These observations indicate that bis(N2 - Alkanoyl-N6 -L-Lysyl-Ethyl Ester) Oxalyl Amides gels as delivery vehicle for nonsteroidal drug molecules and also show that the release profiles for such systems can be fine-tuned by the correct choice of gelatorsolvent combination. Key Words: Organogel, Organogelator, Drug Release, Naproxene, L-Lysine, SEM, NSAID’s.
Novel gemini organogelators based on L-lysine, in which two L-lysine amino acides are linked by oxalyl amide from it’s N6 amino groups through the amide bond, have been simply and effectively synthesized, and their organogelation abilities and thermal stabilities have been investigated. Bis(N2 -Alkanoyl-N6 -L-Lysyl-Ethyl Ester) Oxalyl Amides derivatives with different chain lenght alkanoyl groups at N2-Lysine moiety (4-6: N2 -Alkanoyl=lauroyl, miristoyl, palmitoyl), as a novel LMWGs for pharmaceutical organic fluids have been explored to develop drug depot systems and illustrated for novel dermal and topical drug delivery vehicle for nonsteroidal drug molecule Naproxene. FAE’s (Faty acid ethyl and isopropyl esters) which have different chain length, liquid paraffin, 1,2-propanediol, 1-decanol have been chosen as a biocompatible organic fluids which are used in cosmetic industry. Naproxene(Npx), acting as a model drug, was entrapped in the supramolecular organogels. The release behavior of Npx molecules in the supramolecular organogels was investigated by using UV–vis spectroscopy. The influence of concentration of the organogelator and drug, pH values of the accepting media, and nature of solvent (different FAE’s, Liquid Paraffin, 1,2-Propanediol, 1-Decanol ) on the release behavior of Npx was investigated under static conditions. The results indicated that the release rate of Npx in the supramolecular organogels was effectively retarded with an increase of the organogelator concentration. Also, the release amount of Npx increased with increasing of the Npx content but this didn’t the change release rate of Npx by increasing of it’s amount. Furthermore, the release behavior of Npx was found to be different at various pH values in buffers as accepting media. The study of the release kinetics indicated that the release behavior of Npx was in accord with the Higuchi equation and the diffusion-controlled mechanism involved in the Fickian model. These observations indicate that bis(N2 - Alkanoyl-N6 -L-Lysyl-Ethyl Ester) Oxalyl Amides gels as delivery vehicle for nonsteroidal drug molecules and also show that the release profiles for such systems can be fine-tuned by the correct choice of gelatorsolvent combination. Key Words: Organogel, Organogelator, Drug Release, Naproxene, L-Lysine, SEM, NSAID’s.
Açıklama
Anahtar Kelimeler
Organojel, Organogel, Organojelatör, Organogelator, İlaç salım, Drug release, Naproksen, Naproxene, L-Lizin, L-Lysine, SEM, NSAID’s
