Indomethacin is an anti-inflammatory drug with serious side effects on the gastrointestinal tract. Encapsulation of the drug into nanocapsules allowed the therapeutic activity of the drug to be maintained while eliminating side effects . Freeze-drying the suspension of indomethacin-loaded nanocapsules provided a dosage form that was stable over several years. The physical stability and inhibitory activity of the indomethacin nanocapsules on inflammation and platelet aggregation were evaluated . The encapsulation of approximately 99% indomethacin within orally administered /3CD-C-6 nanocapsules with an average size of 194 nm protected against both gastric and intestinal ulceration was compared with an oral administration of an aqueous solution of Indocid (R) . The relative bioavailability was increased by this encapsulation. PLA nanoparticles containing indomethacin were prepared by interfacial deposition of PLA following acetone displacement from a dichloromethane acetone solution toward an aqueous phase .
Indomethacin loaded poly(D, L-lactide) nanocapsules were investigated after intravenous and rectal administration to rabbits . A rebound of indomethacin plasma concentrations attributed to enterohepatic circulation of indomethacin was observed with all preparations. Following i.v. infusions, results showed that the poly(D, L-lactide) nanocapsules altered the pharmacokinetics of indomethacin in ways that accelerated the extravascular distribution by enhancing the capture of the colloidal carrier by the liver and, at the same time, modifying the elimination rate of indomethacin. Bioavailability and tolerance of indomethacin as polymeric nanocapsules in humans were investigated .
The capacity for increasing the corneal penetration of drugs was investigated for three different colloidal carriers, namely, nanoparticles and nanocapsules made of poly-e-caprolactone and submicrometer emulsions . The three systems differed in their inner structure and composition, but with a similar size (200-250 nm) and a negative superficial charge (—16 to —42 mV). Release of the encapsulated indomethacin occurred very rapidly upon high dilution in a buffered medium and was independent of the composition of the system.
Influence of benzyl benzoate as oil core on the physico-chemical properties of spray-dried powders from polymeric nanocapsules containing indomethacin was studied . Intestinal toxicity exerted by indomethacin was compared to that induced by copper-indomethacinate, free or associated to zwitterionic phospholipids . A single high dose of indomethacin (15 or 20 mg/kg), copper-indomethacinate (15 or 20 mg/kg), or copper-indomethacinate liposomes or nanocapsules (15 mg/kg) was orally administered. Anti-inflammatory activity of the drugs was investigated using the carrageenan-induced paw edema model. Indomethacin induced penetrating ulcerations of the intestine that were maximal at hour 24.
The loading of drugs into ultrafine host vesicles or colloidal capsules in the nanometer size range was an acknowledged technique for the optimization of controlled drug delivery [848, 849]. Two methods for the determination of cisplatin-loaded polyalkylcyanoacrylate nanoparticles were developed . The analyses were carried out by high performance liquid chromatography (HPLC) with UV detection and results were checked with those obtained by inductively coupled plasma-optical emission spectrometry. A nanocapsule formulation with a hydrophilic core was applied to the oral administration of salmon calcitonin in rats .
The preparation from w/o microemulsion of polybutyl-cianacrylate nanocapsules incorporating doxorubicine was optimized applying a multivariate experimental design [852, 853]. Overcoming multidrug resistance with the aid of doxorubicin loaded onto the polyisobutylcyanoacry-late nanoparticles was associated with an increased intra-cellular drug content . Multidrug-resistance bypass in cells exposed to doxorubicin-loaded nanosphere was studied in the absence of endocrtosis . The effect of isobutylcyanoacrylate nanoparticles, in the size range of 100-220 nm, on the disposition of doxorubicin was investigated .
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