A toxicological and pharmacological study of ibuprofen guaiacol ester (AF 2259) in the rat

Cioli, V.; Putzolu, S; Rossi, Vincent M.; Corradino, C

doi:10.1016/0041-008x(80)90203-3

Cited by 33 publications

(14 citation statements)

References 2 publications

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“…Cioli et al [14] have investigated the toxicological and pharmacological profile of ibuprofen guiacol ester 1. The gastrointestinal toxicity, behavioural disorders and acute toxicity of the ester were much reduced in comparison to ibuprofen.…”

Section: Prodrugs Of Nsaidsmentioning

confidence: 99%

Prodrug Designing of NSAIDs

Halen¹,

Murumkar²,

Giridhar³

et al. 2009

MRMC

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Non-steroidal anti-inflammatory drugs (NSAIDs), commonly used for the treatment of chronic inflammatory diseases suffer from several undesired side effects, the most important being gastrointestinal (GI) irritation and ulceration. The prodrug designing is one of the several strategies used to overcome this drawback. The rationale behind the prodrug concept is to achieve temporary blockade of the free carboxylic group present in the NSAIDs till their systemic absorption. In this paper, a review on the concept of prodrugs designing of NSAIDs to improve their efficacy and reduce the toxicity is being presented.

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Section: Prodrugs Of Nsaidsmentioning

confidence: 99%

Prodrug Designing of NSAIDs

Halen¹,

Murumkar²,

Giridhar³

et al. 2009

MRMC

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“…Fetal malformation should not be expected since in animals embryotoxicity prevails over teratogenicity. Lonid amine is not likely to produce a pronounced diuretic activity in man since in animals it is about 40 times less active than chlorothiazide [8] whereas the clinical doses are only 5-10 times higher. As far as neph rotoxicity is concerned, it was associated with an in crease of serum urea and creatinine in monkeys.…”

Section: Discussionmentioning

confidence: 99%

“…Lonidamine lacks the characteristic effects of anti proliferative antineoplastic drugs: white and red cell reduction, hair loss, thymus and spleen atrophy, gas trointestinal lesions, inhibition of some inflammatory processes [8,9]. It is also devoid of mutagenicity in the routine tests [10]; it is well known that this, too, is a property characteristic of antineoplastics which inter fere with the genetic make-up of the cells.…”

Section: Lack O F Effects Reflecting a Primary Action On Cell Divisiomentioning

confidence: 99%

“…It is also devoid of mutagenicity in the routine tests [10]; it is well known that this, too, is a property characteristic of antineoplastics which inter fere with the genetic make-up of the cells. Lethal and sublethal doses of Lonidamine produce prostration, anorexia and clonic convulsions; vomiting and renal failure are also observed in monkeys [9], Antitumor Activity is Correlated with Antispermatogenic and Embryotoxic Effects These latter effects are produced at doses overlap ping or lower than the antitumoral ones [8,[11][12][13][14][15][16][17][18][19], Spermatogenesis is blocked at a relatively advanced stage of cell differentiation corresponding to either the spermatocytes or the spermatids depending on the animal species; spermatogonia and Leydig's cells are unaffected. In this respect Lonidamine and its active analogs are similar although the effective doses may differ considerably [12,19,20], Embryotoxicity preferentially manifests itself in a precise phase of embryofetal development corresponding to the 9th day of rat pregnancy; teratogenicity is also observed although it is impossible to separate it from the cmbryolethal effect [ 18], Lonidamine or its active analogs do not reduce female fertility nor do they alter the estrous cycle [21].…”

Section: Lack O F Effects Reflecting a Primary Action On Cell Divisiomentioning

confidence: 99%

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Lonidamine, a New Approach to Cancer Therapy

Caputo

Silvestrini

1984

Oncology

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The experimental and theoretical bases for the use of Lonidamine in cancer therapy are reviewed and discussed. In murine tumors Lonidamine has a narrow spectrum of antitumor effects. It lacks the characteristic properties of antiproliferative drugs, as well as other important pharmacological actions, with the exception of antispermatogenic and embryotoxic effects which are closely related to the antitumor ones. Lonidamine appears not to affect the cell division processes. Available data instead show that it specifically affects the condensed or oxidized mitochondrion; since tumor cells have a mitochondrially bound hexokinase, both respiration and glycolysis are decreased. There is some evidence that hyperthermia, X rays and some chemotherapeutic agents, when used in combination with Lonidamine, increase the response of tumor cells or systems to this drug.

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“…The mucosal surface was washed with saline and an image of the stomach captured using a CCD scanner at a resolution of 2,400 DPI. The ulcerogenic response was calculated using the method of Cioli et al (19) and the ulcer index determined. The ulcer area was measured and scored according to Table I.…”

Section: Pharmacological Studymentioning

confidence: 99%

Reduced Ulcerogenic Potential and Antiarthritic Effect of Chitosan–Naproxen Sodium Complexes

Ghosh

Bhise²,

Paradkar

et al. 2012

AAPS PharmSciTech

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Abstract. The purpose of this research was to address the utility of naproxen sodium-chitosan spray-dried complexes for antiulcer and antiarthritic activities. The cold stress technique was used to examine the ulcerogenic potential of naproxen sodium (NPX) and spray-dried formulations in the different doses. The ulcerations reduced with the dose of spray-dried complexes of naproxen sodium and chitosan. The conspicuous hemorrhagic lesions were visible in the morphological features of the animal treated with naproxen 50 mg/kg (p.o.). Thus, the results suggest that the spray-dried naproxen sodium-chitosan complex (NPXF) was not corrosive to the gastric mucosa at high doses of 50, 100, and 200 mg/kg (p.o.) under stressful conditions. It is evident from the present investigation that NPXF does not possess any ulcerogenic potential in comparison to naproxen which, under stressful conditions, led to the hypersecretion of HCl, culminating to petichial hemorrhages in the gastric mucosa of the animals. The biphasic pattern was observed in the various arthritic parameters. The rise in paw volume, joint diameter, WBC count, arthritis score, and fall in body weight was significantly ameliorated in the animals treated with NPXF (5, 10, and 20 mg/kg, p.o). At the end of the study, slight erythema was visible in the naproxen-treated animals. However, no erythema, redness, or ulcers were visible in the animals treated with NPXF. Thus, the direct compression properties and reduced ulcerogenic activity, combined with the demonstrated solubilizing power and analgesic effect enhancer ability toward the drug, make naproxen sodium-chitosan spray-dried complexes particularly suitable for developing a reduced-dose, fast-release, solid oral dosage form of naproxen.

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A toxicological and pharmacological study of ibuprofen guaiacol ester (AF 2259) in the rat

Cited by 33 publications

References 2 publications

Prodrug Designing of NSAIDs

Prodrug Designing of NSAIDs

Lonidamine, a New Approach to Cancer Therapy

Reduced Ulcerogenic Potential and Antiarthritic Effect of Chitosan–Naproxen Sodium Complexes

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