Enhanced Bioavailability and Bone Health: Transdermal Delivery of Calcitonin Transfersomes Gel Reduces Osteoclast Numbers and Increases Bone Calcium in Ovariectomized Rats
نویسندگان
1 Laboratory of Pharmacology and Toxicology, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
2 Laboratory of Microbiology and Pharmaceutical Biotechnology Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
3 Laboratory of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
4 Laboratory of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
doi
10.26655/JMCHEMSCI.2024.12.23چکیده
Salmon calcitonin (sCT) is a peptide hormone primarily used for osteoporosis due to the ability to regulate calcium and bone metabolism. However, its therapeutic efficacy through conventional routes of administration such as injection is limited by poor bioavailability, rapid degradation, and its invasive nature. Transdermal delivery systems, such as transfersome gels, offer a promising alternative by enhancing absorption through the skin. Therefore, this study aimed to evaluate the relative bioavailability and pharmacodynamic effects of transdermally administered sCT transfersomes gel in female rats. Pharmacokinetic tests of the transfersomes gel containing sCT were conducted on female Sprague-Dawley rats. A total of 10 rats were divided into 2 groups (n = 5 each) and received a single dose of sCT (4 µg/200 g). Group 1 was treated with transdermally administered transfersomes gel, and Group 2 received subcutaneously administered injection solution. As sCT concentration versus time was calculated, area under the curve (AUC) was determined. The pharmacodynamic analysis was conducted by counting the number of osteoclasts using TRAP staining and analyzing calcium levels in rats’ tibia bone using Atomic Absorption Spectroscopy (AAS). In the pharmacokinetic test of transdermally administered sCT transfersomes gel, there was an increase in relative bioavailability by 144.32% compared to the subcutaneously administered injection solution. The results of pharmacodynamic analysis showed that sCT transfersomes gel increased calcium levels in rat tibia bone and reduced the number of osteoclasts in ovariectomized (Ovx) samples. This showed that sCT transfersomes gel could improve the relative bioavailability and prevent osteoporosis in Ovx rats.