Liposomal Encapsulation for Systemic Delivery of Propranolol via Transdermal Iontophoresis Improves Bone Microarchitecture in Ovariectomized Rats

Abstract

The stimulatory effects of liposomal propranolol (PRP) on proliferation and differentiation of human osteoblastic cells suggested that the prepared liposomes-encapsulated PRP exerts anabolic effects on bone in vivo. Iontophoresis provides merits such as sustained release of drugs and circumvention of first pass metabolism. This study further investigated and evaluated the anti-osteoporotic effects of liposomal PRP in ovariectomized (OVX) rats via iontophoresis. Rats subjected to OVX were administered with pure or liposomal PRP via iontophoresis or subcutaneous injection twice a week for 12 weeks. Changes in the microarchitecture at the proximal tibia and the fourth lumbar spine were assessed between pure or liposomal PRP treated and non-treated groups using micro-computed tomography. Administration of liposomal PRP at low dose (0.05 mg/kg) via iontophoresis over 2-fold elevated ratio between bone volume and total tissue volume (BV/TV) in proximal tibia to 9.0% whereas treatment with liposomal PRP at low and high (0.5 mg/kg) doses via subcutaneous injection resulted in smaller increases in BV/TV. Significant improvement of BV/TV and bone mineral density (BMD) was also found in the fourth lumbar spine when low-dose liposomal PRP was iontophoretically administered. Iontophoretic low-dose liposomal PRP also elevated trabecular numbers in tibia and trabecular thickness in spine. Enhancement of bone microarchitecture volumes has highlighted that liposomal formulation with transdermal iontophoresis is promising for PRP treatment at the lower dose and with longer duration than its clinical therapeutic range and duration to exhibit optimal effects against bone loss in vivo.

Protective Effect of Acteoside on Ovariectomy-Induced Bone Loss in Mice

“…Therefore, the data obtained from the micro-CT and biochemical detection were believed to be more meaningful and comprehensive for the diagnosis of osteoporosis. In the present study, acteoside dose-dependently (20, 40, and 80 mg/kg/day) improved the BMD in OVX mice, and most of the variables in the micro-CT experiment were significantly ameliorated, including the reduction of BMC, TMC, BVF, Tb.N, and Tb.Th in OVX mice, which was consistent with the published data [27], whereas the increment of Tb.Sp was totally reversed; moreover, in parallel with the micro-CT findings, the biomechanical parameters, including the maximal load and stiffness, were also significantly enhanced by acteoside treatment. Therefore, our data implied the therapeutic effect of acteoside on bone microarchitecture of OVX mice.…”

Chronic psychosocial stress disturbs long-bone growth in adolescent mice

“…Furthermore, it was shown that SNS signaling in osteoblasts via βARs acts catabolically on bone by suppressing bone formation and enhancing bone resorption ( Takeda et al, 2002 ; Takeda and Karsenty, 2008 ). Therefore, administration of βAR-blockers leads to enhanced bone formation in both mice ( Takeda and Karsenty, 2008 ; Yirmiya et al, 2006 ; Teong et al, 2017 ) and humans ( Pasco et al, 2004 ; Toulis et al, 2014 ). However, because osteoblast numbers and activity did not differ in our study, βAR signaling in osteoblasts may be unaltered following CSC, as indicated by the unchanged TH expression level at the metaphyseal bone region.…”

Green Tea Catechin (-)-Epigallocatechin-3-Gallate (EGCG) Facilitates Fracture Healing

“…For scanning, the scan settings were an aluminum filter of 0.5 mm, 9 µm scanning resolution, X-ray voltage of 50 kV, X-ray current of 200 mA, and exposure time of 600 ms. The analysis began from the proximal tibia and through the whole fracture site until the distal tibia [19,[21][22][23][24][25][26].…”