Biopharmaceutical and physicochemicai studies on reserpine-polyvinylpyrrolidone coprecipitates

Stupak, Elliot I.; Rosenberg, Howard A.; Bates, Theodore R.

doi:10.1007/bf01070945

Cited by 15 publications

(9 citation statements)

References 14 publications

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“…Dioscin (2) (200 mg) was isolated from fraction 7 by elution with the mixtures of CHCl3 and MeOH (3:1) and was purified by further Si gel column chromatography by elution with the mixtures of CHCl3, MeOH, and H2O (8:2:0.2). The structure of dioscin (2) was determined by data comparison (mp, [R]D, UV, IR, 1 H NMR, 13 C NMR, FABMS) with literature values. 47 Cell Cultures.…”

Section: Methodsmentioning

confidence: 99%

Evaluation of the Potential Cancer Chemotherapeutic Efficacy of Natural Product Isolates Employing in Vivo Hollow Fiber Tests

Lantvit

Reyes-Lim

et al. 2002

J. Nat. Prod.

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The hollow fiber test has been developed for the preliminary in vivo assessment of cancer chemotherapeutic efficacy of selected natural products. Using this model, we have established growth conditions for HL-60, HUVEC, Ishikawa, KB, KB-V1, LNCaP, Lu1, MCF-7, Mel2, P-388, and SW626 cells implanted at the intraperitoneal (i.p.) and subcutaneous (s.c.) compartments of athymic mice. Five cytotoxic natural product isolates (2-6) were tested in this model, along with paclitaxel (taxol) (1). Among the compounds tested, dioscin (2) and 13-methoxy-15-oxozoapatlin (3) were found to be active, indicating their potential to function as cancer chemotherapeutic agents. On the other hand, ochraceolide A (4), alpha-lapachone (5), and 2-(1-hydroxyethyl)naphtha[2,3-b]furan-4,9-quinone (6), all of which were significantly cytotoxic to cultured mammalian cells, did not mediate significant responses with the hollow fiber model. In further xenograft studies using KB cells implanted at the subcutaneous site, compound 3 mediated a statistically significant response which was consistent with the response observed at the subcutaneous compartment in the hollow fiber tests. In sum, these studies illustrate the usefulness of the hollow fiber model in natural product drug discovery programs. Preliminary indications of potential therapeutic efficacy can be provided quickly at relatively low expense. Agents capable of mediating a response at the subcutaneous site would appear to warrant greatest attention.

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Section: Methodsmentioning

confidence: 99%

Evaluation of the Potential Cancer Chemotherapeutic Efficacy of Natural Product Isolates Employing in Vivo Hollow Fiber Tests

Lantvit

Reyes-Lim

et al. 2002

J. Nat. Prod.

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“…Recently, 2-(2-ethoxyethoxy)ethanol (Transcutol Ò ) has been investigated as an efficient co-solvent for solubility enhancement of several poorly water-soluble drugs [9][10][11][12][13][14][15]. Various attempts via co-precipitation, solid dispersion and co-solvency approach have been made in order to enhance solubility and dissolution rate enhancement of reserpine [7,8,[16][17][18]. However, the thermodynamics of solubility of reserpine in various {2-(2-ethoxyethoxy)ethanol + water} mixed solvent systems have not been reported in literature.…”

Section: Introductionmentioning

confidence: 99%

“…It has been reported as a poorly watersoluble compound in water and most of the organic solvents [6]. Weak water-solubility of drugs is the main barrier for their formulation development [7,8]. Recently, 2-(2-ethoxyethoxy)ethanol (Transcutol Ò ) has been investigated as an efficient co-solvent for solubility enhancement of several poorly water-soluble drugs [9][10][11][12][13][14][15].…”

Section: Introductionmentioning

confidence: 99%

Thermodynamics of the solubility of reserpine in {{2-(2-ethoxyethoxy)ethanol + water}} mixed solvent systems at different temperatures

Shakeel

Haq

Siddiqui

et al. 2015

The Journal of Chemical Thermodynamics

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Section: In Vivo Hollow Fiber Assay As a Tool For Anticancer Drug Dismentioning

confidence: 99%

“…The resulting precipitate is dissolved in an aqueous solution appropriate for the subsequent biological assay. This method has been used by other laboratories studying the biology of natural products such as reserpine 45 and digitoxin. 46 The dose levels chosen for each test compound are determined by performing acute toxicity tests for each agent as described by the Food and Drug Administration 47 and the NCI Developmental Therapeutics Program.…”

Section: In Vivo Hollow Fiber Assay As a Tool For Anticancer Drug Dis...mentioning

confidence: 99%

Use of the in Vivo Hollow Fiber Assay in Natural Products Anticancer Drug Discovery

Pezzuto

Farnsworth

et al. 2009

J. Nat. Prod.

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The in vivo hollow fiber assay was developed at the National Cancer Institute (NCI) to help bridge the gap between in vitro cell-based assays and human tumor models propagated in immunodeficient mice. The goal was to develop an intermediate assay that could help predict which compounds found active in the 60-cell line panel would be active in a subsequent xenograft system. This was necessary due to the high cost of the traditional xenograft assay in terms of number of animals required, time for assay completion, and financial commitment necessary. To address this problem, investigators of the NCI Developmental Therapeutics Program designed a method of propagating human cancer cells in inert hollow fibers with pores small enough to retain the cancer cells but large enough to permit entry of potential chemotherapeutic drugs, including large proteins and other important substances. Fibers containing proliferating cancer cells are transplanted into the peritoneum or under the skin, the host mice are treated with a test agent and the fibers are subsequently retrieved for analysis of viable cell mass. The assay has been successful in helping investigators from around the world, including our own research group, prioritize compounds active in vitro for further testing in the traditional xenograft system.

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Biopharmaceutical and physicochemicai studies on reserpine-polyvinylpyrrolidone coprecipitates

Cited by 15 publications

References 14 publications

Evaluation of the Potential Cancer Chemotherapeutic Efficacy of Natural Product Isolates Employing in Vivo Hollow Fiber Tests

Evaluation of the Potential Cancer Chemotherapeutic Efficacy of Natural Product Isolates Employing in Vivo Hollow Fiber Tests

Thermodynamics of the solubility of reserpine in {{2-(2-ethoxyethoxy)ethanol + water}} mixed solvent systems at different temperatures

Use of the in Vivo Hollow Fiber Assay in Natural Products Anticancer Drug Discovery

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