In vivo evaluation of a reverse water-in-fluorocarbon emulsion stabilized with a semifluorinated amphiphile as a drug delivery system through the pulmonary route.
The potential of a reverse water-in-fluorocarbon (w-in-FC) emulsion stabilized with a semifluorinated amphiphile, namely C8F17(CH2)11OP(O)[N(CH2CH2)2O]2 (F8H11DMP) for drug delivery through intrapulmonary administration was investigated in the mouse. This study involved assessment of the effect of single or repeated intranasal instillations of a plain emulsion on lung tissue integrity, and evaluation of blood glucose levels in mice treated with an insulin-loaded emulsion. When instilled intranasally to mice, the plain emulsion did not alter lung tissue integrity, as demonstrated by histological staining, and did not induce any airway inflammatory reaction. Treated mice exhibited decreased body weight within the 3-4 days that followed the first emulsion administration, but this decrease was reversible within few days. Mice instilled intranasally with the insulin-loaded emulsion displayed decreased blood glucose levels within the 20 min that followed the administration, thus demonstrating the potential of the reverse w-in-FC emulsion stabilized with F8H11DMP to systemically deliver drugs, including peptides, upon lung administration.
Courrier
H M
HM
UMR 7514, Laboratoire de Chimie Bioorganique, Faculté de Pharmacie, Université Louis Pasteur, 74 Route du Rhin, B.P. 60024, 67401 Illkirch Cedex, France.
Pons
F
F
Lessinger
J M
JM
Frossard
N
N
Krafft
M P
MP
Vandamme
Th F
TF
D000281:Administration, Intranasal; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D001835:Body Weight / Q000187:drug effects; D001992:Bronchoalveolar Lavage Fluid / Q000166:cytology; D016503:Drug Delivery Systems; D004655:Emulsions; D005466:Fluorocarbons / Q000737:chemistry*; D007004:Hypoglycemic Agents / Q000008:administration & dosage / Q000494:pharmacology; D007202:Indicators and Reagents; D007328:Insulin / Q000008:administration & dosage / Q000494:pharmacology; D008168:Lung / Q000378:metabolism*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C
D001786:Blood Glucose; D004655:Emulsions; D005466:Fluorocarbons; D007004:Hypoglycemic Agents; D007202:Indicators and Reagents; D007328:Insulin