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Karvedilolun Çözünürlüğünü Arttırıcı Olarak Jeffamine® Çekirdekli PAMAM Dendrimerler

Yıl 2019, Cilt: 9 Sayı: 1, 130 - 138, 01.03.2019
https://doi.org/10.21597/jist.430007

Öz

Bu çalışmada amacımız Jeffamine® çekirdekli PAMAM dendrimerlerin, biyofarmasötik sınıflandırma sistemi sınıf II ilacı ve alfa 1 engelleyici aktivite ile seçici olmayan bir beta-adrenerjik bloke edici ajan olan karvedilol’ün (CAR) sudaki çözünürlüğü üzerindeki etkisini araştırmaktır. CAR'ın sudaki çözünürlüğü, geleneksel döner şişe tekniği kullanılarak fosfat tamponlu tuz içinde oda sıcaklığında dendrimerler varlığında ölçüldü. Faz çözünürlük çalışmalarından elde edilen sonuçlar, CAR'ın sudaki çözünürlüğünü, dendrimer konsantrasyonuyla neredeyse orantılı olduğunu ve PAMAM dendrimerlerin mevcudiyetinde önemli ölçüde arttığını gösterdi. Bu çalışmalar gösterdi ki, PAMAM dendrimerlerin CAR'nin çözünürlüğünü arttırıcı olarak düşünülebileceğini ve çeşitli formülasyonların geliştirilmesine yardımcı olabileceğini gösterdi.

Kaynakça

  • Abderrezak A, Bourassa P, Mandeville JS, Sedaghat-Herati R, Tajmir-Riahi HA, 2012. Dendrimers bind antioxidant polyphenols and cisplatin drug. PloS one, 7 (3): e33102.
  • Devarakonda B, Otto DP, Judefeind A, Hill RA, de Villiers MM, 2007. Effect of pH on the solubility and release of furosemide from polyamidoamine (PAMAM) dendrimer complexes. International Journal of Pharmaceutics, 345 (1–2): 142-153.
  • Dollery C, 1999. Therapeutic drugs+CD. Elsevier Science Health Science Division.
  • Erturk AS, Gurbuz MU, Tulu M, Bozdogan AE, 2015. Water-soluble TRIS-terminated PAMAM dendrimers: microwave-assisted synthesis, characterization and Cu(ii) intradendrimer complexes. RSC Advances, 5 (74): 60581-60595.
  • Ertürk AS, Gürbüz MU, Tülü M, 2016. The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil. Pharmaceutical Development and Technology, 22 (1): 111-121.
  • Ertürk AS, Tülü M, Bozdoğan AE, Parali T, 2014. Microwave assisted synthesis of Jeffamine cored PAMAM dendrimers. European Polymer Journal, 52: 218-226.
  • Filipowicz A, Wołowiec S, 2011. Solubility and in vitro transdermal diffusion of riboflavin assisted by PAMAM dendrimers. International Journal of Pharmaceutics, 408 (1–2): 152-156.
  • Gürbüz MU, Ertürk AS, Tülü M, 2016. Synthesis of surface modified TREN cored PAMAM dendrimers and their effects on the solubility of sulfamethoxazole (SMZ) as an analogue antibiotic drug. Pharmaceutical Development and Technology, 22 (5): 678-689.
  • Higuchi T, Connors KA, 1965. Phase-solubility techniques. Advances in Analytical Chemistry and Instrumentation, 4: 117-212.
  • Hirlekar R, Kadam V, 2009. Preparation and characterization of inclusion complexes of carvedilol with methyl-β-cyclodextrin. J Incl Phenom Macrocycl Chem, 63 (3-4): 219-224.
  • Kovačič B, Vrečer F, Planinšek O, 2011. Solid dispersions of carvedilol with porous silica. Chemical and Pharmaceutical Bulletin, 59 (4): 427-433.
  • Milhem OM, Myles C, McKeown NB, Attwood D, D’Emanuele A, 2000. Polyamidoamine Starburst® dendrimers as solubility enhancers. International Journal of Pharmaceutics, 197 (1–2): 239-241.
  • Pamudji JS, Mauludin R, Lestari VA, 2014. Improvement of carvedilol dissolution rate through formation of inclusion complex with β-cyclodextrin. International Journal of Pharmacy and Pharmaceutical Sciences 6(4): 2-7.
  • Sharma A, Jain C, 2010. Preparation and characterization of solid dispersions of carvedilol with PVP K30. Research in Pharmaceutical Sciences, 5 (1): 49.
  • Virmani T, Parvez N, Yadav S, Pathak K, 2007. Solid Inclusion Complexes of Class II Imidazole Derivative With β–Cyclodextrin. Continental Journal of Pharmaceutical Sciences, 1: 1-8.
  • Wei L, Sun P, Nie S, Pan W, 2005. Preparation and Evaluation of SEDDS and SMEDDS Containing Carvedilol. Drug Development and Industrial Pharmacy, 31 (8): 785-794.
  • Wen X, Tan F, Jing Z, Liu Z, 2004. Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin. Journal of Pharmaceutical and Biomedical Analysis, 34 (3): 517-523.
  • Yiyun C, Tongwen X, 2005a. Dendrimers as potential drug carriers. Part I. Solubilization of non-steroidal anti-inflammatory drugs in the presence of polyamidoamine dendrimers. European journal of medicinal chemistry, 40 (11): 1188-1192.
  • Yiyun C, Tongwen X, 2005b. Solubility of nicotinic acid in polyamidoamine dendrimer solutions. European journal of medicinal chemistry, 40 (12): 1384-1389.

Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol

Yıl 2019, Cilt: 9 Sayı: 1, 130 - 138, 01.03.2019
https://doi.org/10.21597/jist.430007

Öz

The aim of this study was to investigate the effect of Jeffamine® core poly(amidoamine) PAMAM dendrimers (JCPDs) on the aqueous solubility of carvedilol (CAR), a Biopharmaceutical Classification System (BCS) Class II drug, and a nonselective beta-adrenegenic blocking agent with alpha 1-blocking activity. The aqueous solubility of CAR was measured in the presence of JCPDs at room temperature in phosphate-buffered saline using traditional rotating bottle technique. Results obtained from the phase solubility studies revealed that the molar aqueous solubility of CAR increased significantly with a proportional increase in the concentration of fourth-generation JCPD, P4.NH2. Likewise, the encapsulation efficiency of JCPD, P4.NH2 improved as its concentration increased and the highest capacity was observed to be 60.75%. Furthermore, the drug binding constant of P4.NH2 (11177.31 ± 0.15 M-1) was found to be fifty times higher than that of β-cyclodextrin (227 M-1), which is the most common studied solubility enhancer excipient for CAR drug. Overall, it can be concluded that PAMAMs, used for the first time in this study as the successful solubility enhancer of CAR, might be helpful and good candidates for the development of various formulations in the future studies.

Kaynakça

  • Abderrezak A, Bourassa P, Mandeville JS, Sedaghat-Herati R, Tajmir-Riahi HA, 2012. Dendrimers bind antioxidant polyphenols and cisplatin drug. PloS one, 7 (3): e33102.
  • Devarakonda B, Otto DP, Judefeind A, Hill RA, de Villiers MM, 2007. Effect of pH on the solubility and release of furosemide from polyamidoamine (PAMAM) dendrimer complexes. International Journal of Pharmaceutics, 345 (1–2): 142-153.
  • Dollery C, 1999. Therapeutic drugs+CD. Elsevier Science Health Science Division.
  • Erturk AS, Gurbuz MU, Tulu M, Bozdogan AE, 2015. Water-soluble TRIS-terminated PAMAM dendrimers: microwave-assisted synthesis, characterization and Cu(ii) intradendrimer complexes. RSC Advances, 5 (74): 60581-60595.
  • Ertürk AS, Gürbüz MU, Tülü M, 2016. The effect of PAMAM dendrimer concentration, generation size and surface functional group on the aqueous solubility of candesartan cilexetil. Pharmaceutical Development and Technology, 22 (1): 111-121.
  • Ertürk AS, Tülü M, Bozdoğan AE, Parali T, 2014. Microwave assisted synthesis of Jeffamine cored PAMAM dendrimers. European Polymer Journal, 52: 218-226.
  • Filipowicz A, Wołowiec S, 2011. Solubility and in vitro transdermal diffusion of riboflavin assisted by PAMAM dendrimers. International Journal of Pharmaceutics, 408 (1–2): 152-156.
  • Gürbüz MU, Ertürk AS, Tülü M, 2016. Synthesis of surface modified TREN cored PAMAM dendrimers and their effects on the solubility of sulfamethoxazole (SMZ) as an analogue antibiotic drug. Pharmaceutical Development and Technology, 22 (5): 678-689.
  • Higuchi T, Connors KA, 1965. Phase-solubility techniques. Advances in Analytical Chemistry and Instrumentation, 4: 117-212.
  • Hirlekar R, Kadam V, 2009. Preparation and characterization of inclusion complexes of carvedilol with methyl-β-cyclodextrin. J Incl Phenom Macrocycl Chem, 63 (3-4): 219-224.
  • Kovačič B, Vrečer F, Planinšek O, 2011. Solid dispersions of carvedilol with porous silica. Chemical and Pharmaceutical Bulletin, 59 (4): 427-433.
  • Milhem OM, Myles C, McKeown NB, Attwood D, D’Emanuele A, 2000. Polyamidoamine Starburst® dendrimers as solubility enhancers. International Journal of Pharmaceutics, 197 (1–2): 239-241.
  • Pamudji JS, Mauludin R, Lestari VA, 2014. Improvement of carvedilol dissolution rate through formation of inclusion complex with β-cyclodextrin. International Journal of Pharmacy and Pharmaceutical Sciences 6(4): 2-7.
  • Sharma A, Jain C, 2010. Preparation and characterization of solid dispersions of carvedilol with PVP K30. Research in Pharmaceutical Sciences, 5 (1): 49.
  • Virmani T, Parvez N, Yadav S, Pathak K, 2007. Solid Inclusion Complexes of Class II Imidazole Derivative With β–Cyclodextrin. Continental Journal of Pharmaceutical Sciences, 1: 1-8.
  • Wei L, Sun P, Nie S, Pan W, 2005. Preparation and Evaluation of SEDDS and SMEDDS Containing Carvedilol. Drug Development and Industrial Pharmacy, 31 (8): 785-794.
  • Wen X, Tan F, Jing Z, Liu Z, 2004. Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin. Journal of Pharmaceutical and Biomedical Analysis, 34 (3): 517-523.
  • Yiyun C, Tongwen X, 2005a. Dendrimers as potential drug carriers. Part I. Solubilization of non-steroidal anti-inflammatory drugs in the presence of polyamidoamine dendrimers. European journal of medicinal chemistry, 40 (11): 1188-1192.
  • Yiyun C, Tongwen X, 2005b. Solubility of nicotinic acid in polyamidoamine dendrimer solutions. European journal of medicinal chemistry, 40 (12): 1384-1389.
Toplam 19 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Kimya Mühendisliği
Bölüm Kimya / Chemistry
Yazarlar

Ali Serol Ertürk 0000-0001-5352-7939

Mustafa Ulvi Gürbüz 0000-0002-8684-5746

Metin Tülü 0000-0001-9791-4922

Abdürrezzak Emin Bozdoğan Bu kişi benim 0000-0003-2102-2906

Yayımlanma Tarihi 1 Mart 2019
Gönderilme Tarihi 2 Haziran 2018
Kabul Tarihi 24 Eylül 2018
Yayımlandığı Sayı Yıl 2019 Cilt: 9 Sayı: 1

Kaynak Göster

APA Ertürk, A. S., Gürbüz, M. U., Tülü, M., Bozdoğan, A. E. (2019). Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol. Journal of the Institute of Science and Technology, 9(1), 130-138. https://doi.org/10.21597/jist.430007
AMA Ertürk AS, Gürbüz MU, Tülü M, Bozdoğan AE. Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol. Iğdır Üniv. Fen Bil Enst. Der. Mart 2019;9(1):130-138. doi:10.21597/jist.430007
Chicago Ertürk, Ali Serol, Mustafa Ulvi Gürbüz, Metin Tülü, ve Abdürrezzak Emin Bozdoğan. “Jeffamine® Core PAMAM Dendrimers As Solubility Enhancer of Carvedilol”. Journal of the Institute of Science and Technology 9, sy. 1 (Mart 2019): 130-38. https://doi.org/10.21597/jist.430007.
EndNote Ertürk AS, Gürbüz MU, Tülü M, Bozdoğan AE (01 Mart 2019) Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol. Journal of the Institute of Science and Technology 9 1 130–138.
IEEE A. S. Ertürk, M. U. Gürbüz, M. Tülü, ve A. E. Bozdoğan, “Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol”, Iğdır Üniv. Fen Bil Enst. Der., c. 9, sy. 1, ss. 130–138, 2019, doi: 10.21597/jist.430007.
ISNAD Ertürk, Ali Serol vd. “Jeffamine® Core PAMAM Dendrimers As Solubility Enhancer of Carvedilol”. Journal of the Institute of Science and Technology 9/1 (Mart 2019), 130-138. https://doi.org/10.21597/jist.430007.
JAMA Ertürk AS, Gürbüz MU, Tülü M, Bozdoğan AE. Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol. Iğdır Üniv. Fen Bil Enst. Der. 2019;9:130–138.
MLA Ertürk, Ali Serol vd. “Jeffamine® Core PAMAM Dendrimers As Solubility Enhancer of Carvedilol”. Journal of the Institute of Science and Technology, c. 9, sy. 1, 2019, ss. 130-8, doi:10.21597/jist.430007.
Vancouver Ertürk AS, Gürbüz MU, Tülü M, Bozdoğan AE. Jeffamine® Core PAMAM Dendrimers as Solubility Enhancer of Carvedilol. Iğdır Üniv. Fen Bil Enst. Der. 2019;9(1):130-8.