ENHANCEMENT OF NASAL ABSORPTION OF CALCITONIN LOADED IN LIPOSOMES

Intranasal administration of calcitonin-containing liposomes in rabbits was investigated to evaluate the in vivo calcitonin absorption performance. Plasma calcitonin concentrations and calcium levels were measured and pharmacokinetic parameters were calculated. The bioavailability of calcitonin resulted from the intranasal delivery formulations demonstrated an order of calcitonin-containing positively charged liposomes > calcitonin-containing negatively charged liposomes > calcitonin solution. The significant enhancement of bioavailability of calcitonin for positively charged liposomes may be due to the charge interaction of positively charged liposomes with the negatively charged mucosa surface. Marked accumulation of positively charged liposomes was found on the negatively charged nasal mucosa surface. The retention of positively charged liposomes on the nasal mucosa resulted in an increase of residence time with high local concentration of calcitonin for increase of absorption.

[1]  Hans Bisgaard,et al.  Bioadhesive microspheres as a potential nasal drug delivery system , 1987 .

[2]  D. Crommelin,et al.  Liposomes and biotherapeutics , 1991, Biotherapy.

[3]  S. Law,et al.  Characterization of calcitonin-containing liposome formulations for intranasal delivery. , 2001, Journal of microencapsulation.

[4]  Claus-Michael Lehr,et al.  In vitro evaluation of mucoadhesive properties of chitosan and some other natural polymers , 1992 .

[5]  V. H. Lee,et al.  Topical ocular drug delivery: recent developments and future challenges. , 1986, Journal of ocular pharmacology.

[6]  K Morimoto,et al.  Enhancement of nasal absorption of insulin and calcitonin using polyacrylic acid gel , 1985, The Journal of pharmacy and pharmacology.

[7]  L. Deftos,et al.  Liposome entrapment enhances the hypocalcemic action of parenterally administered calcitonin. , 1984, Endocrinology.

[8]  A. Perkins,et al.  Evaluation of the clearance characteristics of bioadhesive systems in humans. , 1999, International journal of pharmaceutics.

[9]  K. Taylor.  Book review: Inhalation Delivery of Therapeutic Peptides and Proteins. Adjei AL, Gupta PK, eds. Marcel Dekker, New York , 1997 .

[10]  D. Krohn,et al.  Liposomes in topical drug delivery. , 1982, Investigative ophthalmology & visual science.

[11]  S. Law,et al.  Preparation of desmopressin-containing liposomes for intranasal delivery. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[12]  H. Zia,et al.  The influence of the enhancer dimyristoylphosphatidylglycerol and formulation factors on the nasal absorption of salmon calcitonin. , 1998, Drug delivery.

[13]  V. Lee.  Oral Route of Peptide and Protein Drug Delivery , 1995 .

[14]  A. Pontiroli.  Intranasal administration of calcitonin and of other peptides: Studies with different promoters , 1990 .

[15]  R. Radhakrishnan,et al.  Adhesion of Positively Charged Liposomes to Mucosal Tissues , 1989 .

[16]  H. Zia,et al.  Bioadhesive and formulation parameters affecting nasal absorption , 1996 .

[17]  L. Deftos,et al.  Liposome-entrapped calcitonin and parathyroid hormone are orally effective in rats. , 1991, Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme.