SavedAdd your journal

Journals / Marmara Pharmaceutical Journal / 2017 / Cilt: 21 - Sayı: 2

New-generation Jeffamine® D230 core amine, TRIS and carboxyl- terminated PAMAM dendrimers: Synthesis, characterization and the solubility application for a model NSAID drug Ibuprofen

ALİ SEROL ERTÜRK
Mustafa Ulvi GÜRBÜZ
METİN TÜLÜ
Pages
385–399
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Results showed that synthesized PAMAMs improved the solubility of IBU significantly (30 to 247-fold) with an increasing generation size, and concentration.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Many therapeutically active drugs are poor water soluble and, therefore, bioavailability of these molecules in the living cells is low and a major problem.
📊
Key Findings & Data:In this study, new-generation Jeffamine ® D230 core, amine (NH 2 ), Tris(hydroxymethyl) aminomethane (TRIS), and carboxyl (COOH) terminated poly(amidoamine) PAMAM dendrimers (PAMAMs) were synthesized.
💡
Conclusion & Impact:Results showed that synthesized PAMAMs improved the solubility of IBU significantly (30 to 247-fold) with an increasing generation size, and concentration.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Özet

Many therapeutically active drugs are poor water soluble and, therefore, bioavailability of these molecules in the living cells is low and a major problem. In this study, new-generation Jeffamine ® D230 core, amine (NH 2 ), Tris(hydroxymethyl) aminomethane (TRIS), and carboxyl (COOH) terminated poly(amidoamine) PAMAM dendrimers (PAMAMs) were synthesized. Synthesized new-generation PAMAMs were characterized by 1 H NMR, 13 C NMR, ATR-FTIR, and investigated as solubility enhancer of a sample non-steroidal anti-inflammatory drug (NSAID) Ibuprofen (IBU). The effect of generation size (D2-D4), concentration (0-2.0 mM), and surface functional group (NH 2 , COOH, TRIS) of the synthesized new-generation PAMAMs on the aqueous solubility of IBU was also investigated. The observed solubility enhancement of IBU was in the order of D4.COOH (18.21 mg/mL)> D3.COOH (13.21 mg/mL)> D4.TRIS (10.30 mg/mL)> D2.COOH (8.55 mg/mL)> D3.TRIS (6.04 mg/mL)> D4.NH 2 (4.56 mg/mL)> D3.NH 2 (3.36 mg/mL)> D2.TRIS (2.42 mg/mL)> D2.NH 2 (1.86 mg/mL). Results showed that synthesized PAMAMs improved the solubility of IBU significantly (30 to 247-fold) with an increasing generation size, and concentration.

🔖

Cite This Article

ERTÜRK, A. S., GÜRBÜZ, M. U., TÜLÜ, M. (2017). New-generation Jeffamine® D230 core amine, TRIS and carboxyl- terminated PAMAM dendrimers: Synthesis, characterization and the solubility application for a model NSAID drug Ibuprofen. Marmara Pharmaceutical Journal, Cilt: 21 - Sayı: 2, 385–399. https://ajindex.com/articles/283627

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (13)

  1. Beezer AE, King ASH, Martin IK, Mitchel JC, Twyman LJ, WainCF. Dendrimers as potential drug carriers; encapsulation ofacidic hydrophobes within water soluble PAMAM derivatives.Tetrahedron 2003;59: 3873-80.
  2. Beezer AE, King ASH, Martin IK, Mitchel JC, Twyman LJ, WainCF. Dendrimers as potential drug carriers; encapsulation ofacidic hydrophobes within water soluble PAMAM derivatives.Tetrahedron 2003;59: 3873-80. Carriers D. ReferenceMD Available from: http://www.reference.md/files/D004/mD004337.html [10 Dem 2016]. Carriers D. ReferenceMD Available from: http://www.reference.md/files/D004/mD004337.html [10 Dem 2016].
  3. Felice B, Prabhakaran MP, Rodriguez AP, Ramakrishna S.Drug delivery vehicles on a nano-engineering perspective.Mater Sci Eng C 2014;41: 178-95.
  4. Felice B, Prabhakaran MP, Rodriguez AP, Ramakrishna S.Drug delivery vehicles on a nano-engineering perspective.Mater Sci Eng C 2014;41: 178-95.
  5. Fox ME, Szoka FC, Frechet JMJ. Soluble Polymer Carriersfor the Treatment of Cancer: The Importance of MolecularArchitecture. Acc Chem Res 2009;42: 1141-51.
  6. Fox ME, Szoka FC, Frechet JMJ. Soluble Polymer Carriersfor the Treatment of Cancer: The Importance of MolecularArchitecture. Acc Chem Res 2009;42: 1141-51.
  7. Vandamme TF, Brobeck L. Poly (amidoamine) dendrimers asophthalmic vehicles for ocular delivery of pilocarpine nitrateand tropicamide. J Controlled Release 2005;102: 23-38.
  8. Vandamme TF, Brobeck L. Poly (amidoamine) dendrimers asophthalmic vehicles for ocular delivery of pilocarpine nitrateand tropicamide. J Controlled Release 2005;102: 23-38.
  9. Jia L, Xu J-P, Wang H, Ji J. Polyamidoamine dendrimerssurface-engineered with biomimetic phosphorylcholine aspotential drug delivery carriers. Colloids Surf B 2011;84: 49-54.
  10. Jia L, Xu J-P, Wang H, Ji J. Polyamidoamine dendrimerssurface-engineered with biomimetic phosphorylcholine aspotential drug delivery carriers. Colloids Surf B 2011;84: 49-54.
  11. Malik N, Wiwattanapatapee R, Klopsch R, Lorenz K, Frey H,Weener JW, et al. Dendrimers:: Relationship between structureand biocompatibility in vitro, and preliminary studies on thebiodistribution of 125I-labelled polyamidoamine dendrimersin vivo. J Controlled Release 2000;65: 133-48.
  12. Malik N, Wiwattanapatapee R, Klopsch R, Lorenz K, Frey H,Weener JW, et al. Dendrimers:: Relationship between structureand biocompatibility in vitro, and preliminary studies on thebiodistribution of 125I-labelled polyamidoamine dendrimersin vivo. J Controlled Release 2000;65: 133-48.
  13. Kesharwani P, Jain