Abstract
Objective: In the present study, transdermal nanoemulsion (NE) gel of lovastatin was investigated for its anti-osteoporosis effect on the long bones of rat i.e. tibia.
 Methods: Male wistar rats (n=30, weighing 180-200g) were taken for this study and grouped as: 1) control (normal saline daily), 2) Dex (dexamethasone sodium; 25 mg/kg subcutaneously twice a week), 3) Dex+LNG5 (lovastatin nanoemulsion gel; 5 mg/kg/d transdermally daily), 4) Dex+LNG10 (lovastatin nanoemulsion gel; 10 mg/kg/d transdermally daily), and 5) Dex+ALN (alendronate sodium; 0.03 mg/kg/d orally daily). All the treatments were carried out for 60 d. At the end of the experiment, all animals were anesthetized using diethyl ether and collected blood samples from retro-orbital venous plexus of rats in dry eppendorf tubes followed by the sacrifice of animals by cervical dislocation method and collected tibia bones of both the legs for analysis.
 Results: Bone formation biomarkers (OC: osteocalcin, b-ALP: bone-specific alkaline phosphatase, PINP: N-terminal propeptides of type I procollagen) were significantly improved and resorption biomarkers (CTx: C-terminal cross-linking telopeptides of type-I collagen, TRAcP5b: isoform 5b of tartarate resistant acid phosphatase) were significantly reduced in the LNG5 (p<0.05) and LNG10 (p<0.05) treatment groups when compared to Dex. In vivo anti-osteoporotic results demonstrated the formation of new bone in osteoporotic rat tibias. Biomechanical strength testing demonstrated increased load-bearing capacity of rat tibias in the treated animals in comparison with the osteoporotic group (p<0.05 for LNG5 and p<0.01 for LNG10).
 Conclusion: Thus, the transdermal NE gel formulation of lovastatin demonstrated the greater potential for the treatment of osteoporosis.
Highlights
Osteoporosis is a highly prevalent metabolic bone disorder characterized by low bone mineral density and deteriorated microarchitecture of bone [1]
Biochemical kits specific for alkaline phosphatase (ALP), calcium, phosphorus, total protein (TP), serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), triglyceride and total cholesterol were procured from Accurex, Mumbai, India
Biochemical assay Serum albumin, ALP, calcium, cholesterol, creatinine, glucose, phosphorus, SGOT, SGPT, triglyceride, and total protein levels are represented in table 1
Summary
Osteoporosis is a highly prevalent metabolic bone disorder characterized by low bone mineral density and deteriorated microarchitecture of bone [1]. It often results in hip, distal arm and spine fractures. The increased risk of fragility fractures in osteoporosis poses a threat to life expectancy and quality of life in both men and women. Bone resorption increases in comparison to bone formation, which causes deterioration of bone and leads to osteoporosis. Osteoporosis is of two types, primary and secondary. Glucocorticoid (GC) induced osteoporosis is the most common form of secondary osteoporosis [2]. GC induces apoptosis of both osteoblasts and osteoclasts but increases the resorption process by increasing the life span of pre-existing osteoclasts [3]
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