Poly(alkyl cyanoacrylate) nanocapsules as a delivery system in the rat for octreotide, a long-acting somatostatin analogue.
Poly(alkyl cyanoacrylate) nanocapsules have been used as biodegradable polymeric drug carriers for subcutaneous and peroral delivery of octreotide, a long-acting somatostatin analogue; their ability to reduce insulin secretion or prolactin secretion in response to oestrogens has been studied in adult male rats. The nanocapsules, prepared by interfacial emulsion polymerization of isobutyl cyanoacrylate, were 260 nm in diameter and incorporated 60% of octreotide. Administered subcutaneously, the octreotide-loaded (20 micrograms kg-1) nanocapsules suppressed the insulinaemia peak induced by intravenous glucose overload and depressed insulin secretion over 48 h, preventing the secretory rebound; however, glycaemia was unaffected. In parallel, the plasma octreotide concentration increased 2.7 times. Administered perorally to oestrogen-treated rats, octreotide-loaded nanocapsules (200 and 1000 micrograms kg-1) significantly improved the reduction of prolactin secretion (by 72 and 88%, respectively, compared with 32 and 54% with free octreotide) and slightly increased plasma octreotide level. Thus nanocapsules could be of interest as a biodegradable drug carrier for the administration of octreotide.
Damgé
C
C
Centre Européen d'Etude du Diabète, Strasbourg, France.
Vonderscher
J
J
Marbach
P
P
Pinget
M
M
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002214:Capsules; D003487:Cyanoacrylates / Q000737:chemistry*; D016503:Drug Delivery Systems; D006728:Hormones / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007328:Insulin / Q000097:blood; D008297:Male; D015282:Octreotide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D011388:Prolactin / Q000097:blood; D011863:Radioimmunoassay; D051381:Rats
D001786:Blood Glucose; D002214:Capsules; D003487:Cyanoacrylates; D006728:Hormones; D007328:Insulin; D011388:Prolactin; D015282:Octreotide