Effect of pH on the solubility and release of furosemide from polyamidoamine (PAMAM) dendrimer complexes

Devarakonda, Bharathi; Otto, Daniel P.; Judefeind, Anja; Hill, Ronald A.; Villiers, Melgardt M. de

doi:10.1016/j.ijpharm.2007.05.039

Cited by 119 publications

(56 citation statements)

References 34 publications

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“…DSC analysis of drug-dendrimer complex: The drug-R8 dendrimer complex was prepared at the drug: dendrimer ratio of 1:0.5 by the co-precipitation method, as per previously reported protocols (Devarakonda et al, 2007;Yiyun et al, 2007). Pure 5-FU, pure R8 dendrimer and the drug-R8 dendrimer complex were subjected to DSC analysis by following the method explained above, except the maximum temperature for scanning and heating rate were 300 C and 5 C/min, respectively.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

“…And similar mechanisms might also be at play here, cooperatively enhancing the transdermal permeation of 5-FU. To elucidate further, 5-FU-R8 dendrimer complexes were prepared at a molar ratio of 1:0.5 following a coprecipitation method reported previously (Devarakonda et al, 2007;Yiyun et al, 2007) and skin permeation properties of these complexes was determined. If a complex formed in the presence of excess drug relative to dendrimer, then the melting point, intensity of endothermic peak and charge would also be expected to change in comparison to 5-FU alone.…”

Section: -Fu In Vitro Skin Permeation Studiesmentioning

confidence: 99%

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Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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Enhancing the deposition and permeation of 5-fluorouracil across human epidermis assisted by appropriately charged and well-defined peptide dendrimers was investigated. Peptide dendrimers with arginine as the terminal amino acid and having a range of terminal positive charges (4þ and 16 þ ) were synthesized by solid phase peptide synthesis. Various parameters including effect of peptide dendrimers on the solubility and partition coefficient of 5-FU, degradation of drug in skin as well as deposition and permeation of 5-FU in/through skin were studied. All the tested dendrimers increased the aqueous solubility and partition coefficient of 5-FU with each also significantly (p50.05) enhancing the deposition and permeation of 5-FU in/across human epidermis in a concentration-dependent manner. Of the three peptide dendrimers examined, R8 dendrimer (bearing 8 þ charge derived from four terminal arginines and MW of &1000 Da) showed greatest values for flux, Q 48 (cumulative amount of drug permeated at the end of 48 h) and amount of drug retained in human skin. Furthermore, this study also scrutinized and reports on the likely mechanisms by which peptide dendrimers act as transdermal permeation enhancers.

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Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Section: -Fu In Vitro Skin Permeation Studiesmentioning

confidence: 99%

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

et al. 2013

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“…This compound has a good stability and solubility. It can exist stably in aqueous solution for weeks and in different buffers or pHs, without dissociation (Devarakonda et al, 2007). Tightly bound by means of static electricity effort, the compound can protect DNA from being degraded by enzymes either in or out of cells.…”

Section: Discussionmentioning

confidence: 99%

Anti-angiogenesis effect of generation 4 polyamidoamine/vascular endothelial growth factor antisense oligodeoxynucleotide on breast cancer in vitro

Zhao

Zhang

et al. 2009

J. Zhejiang Univ. Sci. B

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Abstract:Objective: To study the effects of the generation 4 polyamidoamine/vascular endothelial growth factor antisense oligodeoxynucleotide (G4PAMAM/VEGFASODN) compound on the expressions of vascular endothelial growth factor (VEGF) and its mRNA of breast cancer cells and on the inhibition of vascular endothelial cells. Methods: We examined the morphology of G4PAMAM/VEGFASODN compound and its pH stability, in vitro transfection efficiency and toxicity, and the expressions of VEGF and its mRNA. Methyl thiazolyl tetrazolium assay was used to detect the inhibitory function of the compound on vascular endothelial cells. Results: The compound was about 10 nm in diameter and was homogeneously netlike. From pH 5 to 10, it showed quite a buffered ability. The 48-h transfection rate in the charge ratio of 1:40 was 98.76%, significantly higher than that of the liposome group (P<0.05). None of the transfection products showed obvious toxicity on the cells. The expressions of both VEGF protein and its mRNA after G4PAMAM/VEGFASODN transfection decreased markedly. Conclusion: With a low toxicity, high safety, and high transfection rate, G4PAMAM/VEGFASODN could be a promising gene vector. Specifically, it inhibits VEGF gene expression efficiently, laying a basis for further in vivo animal studies.

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“…Similar to diclofenac enteric-coated tablets, a lag time between furosemide ingestion and its appearance in plasma is conceivable because the drug substance is practically insoluble in the acidic medium of the fasted stomach. [46][47][48][49] Therefore, the effect of variability in GET of the nondisintegrated moiety on individual furosemide plasma concentrations following administration of Lasix R tablets was tested. Because no dissolution profile of Lasix R tablets in media simulating fasted gastric fluid was available, dissolution profiles of Lasix R tablets obtained at pH 2.6 were used 49 and combined with the dissolution profile obtained at pH 5.8.…”

Section: Furosemidementioning

confidence: 99%

Evolution of a Detailed Physiological Model to Simulate the Gastrointestinal Transit and Absorption Process in Humans, Part II: Extension to Describe Performance of Solid Dosage Forms

Thelen

Coboeken

Willmann

et al. 2012

Journal of Pharmaceutical Sciences

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Effect of pH on the solubility and release of furosemide from polyamidoamine (PAMAM) dendrimer complexes

Cited by 119 publications

References 34 publications

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

Enhancement in deposition and permeation of 5-fluorouracil through human epidermis assisted by peptide dendrimers

Anti-angiogenesis effect of generation 4 polyamidoamine/vascular endothelial growth factor antisense oligodeoxynucleotide on breast cancer in vitro

Evolution of a Detailed Physiological Model to Simulate the Gastrointestinal Transit and Absorption Process in Humans, Part II: Extension to Describe Performance of Solid Dosage Forms

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