Enhancement of nasal and intestinal calcitonin delivery by the novel Pheroid™ fatty acid based delivery system, and by N-trimethyl chitosan chloride

Therapeutic peptides are highly potent and specific in their functions, but difficulties in their administration require parallel development of viable delivery systems to improve their bioavailability. In this study the potential of a novel lipid-based colloidal delivery system for improving the ab...

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Vydáno v:International journal of pharmaceutics Ročník 385; číslo 1; s. 181 - 186
Hlavní autoři: du Plessis, L.H., Lubbe, J., Strauss, T., Kotzé, A.F.
Médium: Journal Article
Jazyk:angličtina
Vydáno: Netherlands Elsevier B.V 29.01.2010
Témata:
Administration, Intranasal
Administration, Oral
Animals
Calcitonin - administration & dosage
Calcitonin - blood
Calcitonin - chemistry
Calcitonin - pharmacokinetics
Chemistry, Pharmaceutical
Chitosan - chemistry
Colloids
Dosage Forms
Drug Carriers
Fatty Acids - chemistry
Intestinal Absorption
Intestinal drug delivery
Jejunum - metabolism
Liposomes
Male
N-Trimethyl chitosan chloride (TMC)
Nasal drug delivery
Particle Size
Pheroid™ technology
Rats
Rats, Sprague-Dawley
Salmon calcitonin (sCT)
Technology, Pharmaceutical - methods
N-Trimethyl chitosan chloride (TMC)
Nasal drug delivery
Pheroid™ technology
Salmon calcitonin (sCT)
Intestinal drug delivery
ISSN:0378-5173, 1873-3476, 1873-3476
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Shrnutí:Therapeutic peptides are highly potent and specific in their functions, but difficulties in their administration require parallel development of viable delivery systems to improve their bioavailability. In this study the potential of a novel lipid-based colloidal delivery system for improving the absorption of nasally and intestinally administered salmon calcitonin (sCT) was investigated. Two types of delivery vehicles based on Pheroid™ technology was prepared and characterized. Liposome-like bilayer vesicles had a mean diameter of 1.0 μm and microsponges were 1.6 μm. Doses of 10 IU/kg and 500 IU/kg bodyweight sCT were administered intranasally and intestinally to rats, respectively. The obtained absorption enhancement with Pheroid™ vesicles and Pheroid™ microsponges were also compared with the absorption enhancement obtained with N-trimethyl chitosan chloride (TMC). With the inclusion of 0.5% (w/v) TMC the maximum plasma concentration ( C max) of sCT increased from 72.6 ± 6.1 pg/ml to 478.5 ± 6.1 pg/ml after nasal administration. Pheroid™ vesicles and Pheroid™ microsponges increased the C max values of sCT to 262.64 ± 17.1 pg/ml and 202.66 ± 28.6 pg/ml, respectively. The time to reach the maximum concentration ( T max) was also significantly decreased from 35 min to approximately 14 min. Intestinal administration of Pheroid™ formulations increased the C max of sCT from 249.1 ± 21.5 pg/ml to 386.2 ± 45.5 and 432.1 ± 18.9 pg/ml, respectively for Pheroid™ vesicles and Pheroid™ microsponges. TMC increased the C max of sCT to 738.9 ± 277.1 pg/ml. TMC and Pheroid™ technology could offer the potential to significantly improve intranasal and intestinal absorption of sCT and reduce the variability in absorption.
Bibliografie:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ISSN:0378-5173
1873-3476
1873-3476
DOI:10.1016/j.ijpharm.2009.10.031