Author(s): Ashish Srivastava, Ashutosh Mishra, A. K. Rai

Email(s): srivastava457@gmail.com

DOI: 10.5958/0974-360X.2020.00623.X   

Address: Ashish Srivastava1*, Ashutosh Mishra2, A. K. Rai1
1Department of Medicinal Chemistry, Institute of Pharmacy, Pranveer Singh Institute of Technology, Kanpur-209305, Uttar Pradesh, India.
2Acharya Narendra Dev College of Pharmacy, Babhnan, Gonda-271313, Uttar Pradesh, India.
*Corresponding Author

Published In:   Volume - 13,      Issue - 7,     Year - 2020


ABSTRACT:
Objective: To evaluate the effect of diclofenac, indomethacin and ibuprofen conjugates on the bone. Methods: A total of 120 Wistar female rats (aged 50 days, weight 100-150g) were administered intramuscularly with Dexamethasone disodium phosphate (7mg/kg of the body weight, once in a week) to induce the osteoporosis. At the end of the five weeks the rats were treated with Alendronate sodium (30mg/animal/day p.o.), and the prodrugs 1, 2, 3 at the dose of 25, 50 and 100mg/kg p.o. for 30 days Results: The osteoporotic bone demonstrated the signs of improvement through various parameters like serum ALP, bone weight, length, diameter, bone ash, calcium, phosphorus and bone mineral density. Conclusion: The results confirm that these prodrugs have the potential for the improvement of osteoporotic bones.


Cite this article:
Ashish Srivastava, Ashutosh Mishra, A. K. Rai. NSAIDs-Alendronate based Prodrug for Bone specific drug Targeting. Research J. Pharm. and Tech. 2020; 13(7): 3520-3523. doi: 10.5958/0974-360X.2020.00623.X

Cite(Electronic):
Ashish Srivastava, Ashutosh Mishra, A. K. Rai. NSAIDs-Alendronate based Prodrug for Bone specific drug Targeting. Research J. Pharm. and Tech. 2020; 13(7): 3520-3523. doi: 10.5958/0974-360X.2020.00623.X   Available on: https://rjptonline.org/AbstractView.aspx?PID=2020-13-7-83


REFERENCES:
1. Arns, S.; Gibe, R.; Moreau, A.; Monzur Morshed, M.; Young, R. N. Design and synthesis of novel bone-targeting dual-action pro-drugs for the treatment and reversal of osteoporosis. Bioorganic and Medicinal Chemistry. 2012,20, 2131-2140.
2. Farrell, K. B.; Karpeisky, A.; Thamm, D. H.; Zinnen, S. Bisphosphonate conjugation for bone specific drug targeting. Bone Reports. 2018,9, 47-60.
3. Bartl, R.; Gradinger, R. Aktuelle Diagnostik und Therapie der Osteoporose auf der Basis der. European Guidance 2008. Der Orthopäde. 2009,38, 365-380.
4. Xie, H.; Chen, G.; Young, R. N. Design, Synthesis, and Pharmacokinetics of a Bone-Targeting Dual-Action Prodrug for the Treatment of Osteoporosis. J. Med. Chem. 2017,60, 7012-7028.
5. Blume, S. W.; Curtis, J. R. Medical costs of osteoporosis in the elderly Medicare population. Osteoporosis International 2011,22, 1835-1844.
6. Ossipov, D. A. Bisphosphonate-modified biomaterials for drug delivery and bone tissue engineering. Expert Opinion on Drug Delivery 2015,12, 1443-1458.
7. Low, S. A.; Kopeček, J. Targeting polymer therapeutics to bone. Advanced Drug Delivery Reviews 2012,64, 1189-1204.
8. Ossipov, D.; Kootala, S. Bisphosphonate-Immobilized Biomaterials for Bone Engineering and Curing of Bone Diseases. In The World Scientific Encyclopedia of Nanomedicine and Bioengineering II, World Scientific: 2017; Vol. Volume 9, pp 323-342.
9. Uludag, H. Bisphosphonates as a Foundation of Drug Delivery to Bone. Current Pharmaceutical Design 2002,8, 1929-1944.
10. Cole, L. E.; Vargo-Gogola, T.; Roeder, R. K. Targeted delivery to bone and mineral deposits using bisphosphonate ligands. Advanced Drug Delivery Reviews 2016,99, 12-27.
11. Erez, R.; Ebner, S.; Attali, B.; Shabat, D. Chemotherapeutic bone-targeted bisphosphonate prodrugs with hydrolytic mode of activation. Bioorganic and Medicinal Chemistry Letters 2008,18, 816-820.
12. Bauss, F.; Esswein, A.; Reiff, K.; Sponer, G.; Müller-Beckmann, B. Effect of 17β-estradiol-bisphosphonate conjugates, potential bone-seeking estrogen pro-drugs, on 17β-estradiol serum kinetics and bone mass in rats. Calcified Tissue International 1996,59, 168-173.
13. Fujisaki, J.; Tokunaga, Y.; Takahashi, T.; Kimura, S.; Shimojo, F.; Hata, T. Osteotropic Drug Delivery System (ODDS) Based on Bisphosphonic Prodrug. V. Biological Disposition and Targeting Characteristics of Osteotropic Estradiol. Biological and Pharmaceutical Bulletin 1997,20, 1183-1187.
14. Fujisaki, J.; Tokunaga, Y.; Takahashi, T.; Shimojo, F.; Kimura, S.; Hata, T. Osteotropic Drug Delivery System (ODDS) Based on Bisphosphonic Prodrug. IV Effects of Osteotropic Estradiol on Bone Mineral Density and Uterine Weight in Ovariectomized Rats. Journal of Drug Targeting 1998,5, 129-138.
15. Page, P. C. B.; McKenzie, M. J.; Gallagher, J. A. Novel Synthesis of Bis (phosphonic acid)− Steroid Conjugates. The Journal of Organic Chemistry 2001,66, 3704-3708.
16. Bulman Page, P. C.; Moore, J. P. G.; Mansfield, I.; McKenzie, M. J.; Bowler, W. B.; Gallagher, J. A. Synthesis of bone-targeted oestrogenic compounds for the inhibition of bone resorption. Tetrahedron 2001,57, 1837-1847.
17. Morioka, M.; Kamizono, A.; Takikawa, H.; Mori, A.; Ueno, H.; Kadowaki, S.-i.; Nakao, Y.; Kato, K.; Umezawa, K. Design, synthesis, and biological evaluation of novel estradiol–bisphosphonate conjugates as bone-specific estrogens. Bioorganic and Medicinal Chemistry 2010,18, 1143-1148.
18. Gil, L.; Han, Y.; Opas, E. E.; Rodan, G. A.; Ruel, R.; Seedor, J. G.; Tyler, P. C.; Young, R. N. Prostaglandin E2-bisphosphonate conjugates: potential agents for treatment of osteoporosis. Bioorganic and Medicinal Chemistry 1999,7, 901-919.
19. Yewle, J. N.; Puleo, D. A.; Bachas, L. G. Bifunctional bisphosphonates for delivering PTH (1-34) to bone mineral with enhanced bioactivity. Biomaterials 2013,34, 3141-3149.
20. Yang, Y.; Bhandari, K. H.; Panahifar, A.; Doschak, M. R. Synthesis, Characterization and Biodistribution Studies of 125I-Radioiodinated di-PEGylated Bone Targeting Salmon Calcitonin Analogue in Healthy Rats. Pharmaceutical Research 2014,31, 1146-1157.
21. Bhandari, K. H.; Newa, M.; Uludag, H.; Doschak, M. R. Synthesis, characterization and in vitro evaluation of a bone targeting delivery system for salmon Calcitonin. International Journal of Pharmaceutics 2010,394, 26-34.
22. Bhandari, K. H.; Newa, M.; Chapman, J.; Doschak, M. R. Synthesis, characterization and evaluation of bone targeting salmon calcitonin analogs in normal and osteoporotic rats. Journal of Controlled Release 2012,158, 44-52.
23. Doschak, M. R.; Kucharski, C. M.; Wright, J. E. I.; Zernicke, R. F.; Uludaǧ, H. Improved Bone Delivery of Osteoprotegerin by Bisphosphonate Conjugation in a Rat Model of Osteoarthritis. Molecular Pharmaceutics 2009,6, 634-640.
24. Houghton, T. J.; Tanaka, K. S. E.; Kang, T.; Dietrich, E.; Lafontaine, Y.; Delorme, D.; Ferreira, S. S.; Viens, F.; Arhin, F. F.; Sarmiento, I.; Lehoux, D.; Fadhil, I.; Laquerre, K.; Liu, J.; Ostiguy, V.; Poirier, H.; Moeck, G.; Parr, T. R.; Far, A. R. Linking Bisphosphonates to the Free Amino Groups in Fluoroquinolones: Preparation of Osteotropic Prodrugs for the Prevention of Osteomyelitis. J. Med. Chem. 2008,51, 6955-6969.
25. Sedghizadeh, P. P.; Sun, S.; Junka, A. F.; Richard, E.; Sadrerafi, K.; Mahabady, S.; Bakhshalian, N.; Tjokro, N.; Bartoszewicz, M.; Oleksy, M.; Szymczyk, P.; Lundy, M. W.; Neighbors, J. D.; Russell, R. G. G.; McKenna, C. E.; Ebetino, F. H. Design, Synthesis, and Antimicrobial Evaluation of a Novel Bone-Targeting Bisphosphonate-Ciprofloxacin Conjugate for the Treatment of Osteomyelitis Biofilms. J. Med. Chem. 2017,60, 2326-2343.
26. Hirabayashi, H.; Takahashi, T.; Fujisaki, J.; Masunaga, T.; Sato, S.; Hiroi, J.; Tokunaga, Y.; Kimura, S.; Hata, T. Bone-specific delivery and sustained release of diclofenac, a non-steroidal anti-inflammatory drug, via bisphosphonic prodrug based on the Osteotropic Drug Delivery System (ODDS). Journal of Controlled Release 2001,70, 183-191.
27. Padmanabhan. K, Jibi Paul, Sudhakar. S, Senthil Selvam. P, Sathya Priya. V, Veena Kirthika. S. Which is more prevalent among the female population - Osteopenia or Osteoporosis? A cross sectional study. Research J. Pharm. and Tech. 2019; 12(3): 1163-1168.
28. V. I. Strukov, A. I. Kislov, N. V. Eremina, G. P. Deriabina, M. Yu. Sergeeva-Kondrachenko, A. Yu. Antropov, Ya. V. Kuzmina, K. R. Tayrova, E. V. Petrova8, D. G. Elistratov, O. V. Strukova-Jones. The use of Bone Tissue Non-Steroid Anabolizators in Treatment of Osteoporosis. Research J. Pharm. and Tech. 2019; 12(5):2195-2199.
29. Tapan Kumar Giri, Ravikant Sahu, Kulesh Kumar, Amit Alexander, Ajazuddin, Hemant Badwaik, and Dulal Krishna Tripathi. In-vitro quality control measurement of some commercially available sustained release tablet containing diclofenac sodium. Research J. Pharm. and Tech. 5(5): May2012; Page 687-690.
30. Kulwinder Singh, Monika, Neelam Verma. Gastrointestinal and Cardiovascular Risks of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs): Time to Translate Knowledge into Practice. Research J. Pharm. and Tech. 7(5): May, 2014; Page 575-580.
31. Bhagyashri T. Sakat, R B. Sakhare, U C. Suryvanshi, P. S. Kore, . S. K. Mohite, . C. S. Magdum. Osteoporosis: The Brittle Bone. Asian J. Pharm. Res. 2018; 8(1):39-43.
32. Ghanshyam Dhalendra, Trilochan Satapathy, Amit Roy. Animal Models for Inflammation: A Review. Asian J. Pharm. Res. 3(4): Oct. - Dec.2013; Page 207-212.
33. Monika Gaba, Punam Gaba, Sarbjot Singh, Neelima Dhingra. Inhibition of LFA-1/ICAM-1 Interaction: A Therapeutic Strategy for Surmounting Inflammation. Asian J. Pharm. Res. 5(1): Jan.-Mar. 2015; Page 37-47.
34. Nitin Mahurkar, Sayeed ul hasan S.M. Antiulcer Activity of Commicarpus chinensis in Ethanol and Aspirin Induced Ulcers. Asian J. Pharm. Res. 4(3): July-Sept. 2014; Page 119-122.
35. Nitin Mahurkar, S.M. Sayeed ul Hasan. Synergistic Antiulcer Effect of Melatonin and Esomeprazole Combination in Pylorus Ligation, Ethanol, Aspirin induced Peptic Ulcers. Asian J. Pharm. Res. 5(1): Jan.-Mar. 2015; Page 10-14.
36. El harti Jaouad, Ansar M’hammed, Lmimouni Badr, Benomar Ali, Taoufik Jamal. Synthesis and Scolicidal Activity of some Potential Prodrugs of Albendazole. Research J. Pharm. and Tech. 5(11): Nov. 2012; Page 1442-1445.
37. Kalyani Dewangan, Kushagra Nagori, Mukesh Sharma, Ajay Singh, Sandhya Chandrakar, Vandana Devi Sahu, Garima Sharma, Sujata Gupta, Harsha Solanki, Manisha Majumdar, D. K. Tripathi, Amit Alexander, Ajazuddin. Formulation, evaluation and release studies of Indomethacin Suppositories. Research J. Pharm. and Tech. 2016; 9(7):942-944.
38. Arfeen M, Bhagat S, Patel R, Prasad S, Roy I, Chakraborti AK, et al. Design, synthesis and biological evaluation of 5-benzylidene-2-iminothiazolidin-4-ones as selective GSK-3β inhibitors. Eur J Med Chem. 2016 Oct 4; 121:727–36.
39. Bhagat S, Arfeen M, Adane L, Singh S, Singh PP, Chakraborti AK, et al. Guanylthiourea derivatives as potential antimalarial agents: Synthesis, in vivo and molecular modelling studies. Eur J Med Chem. 2017 Jul 28; 135:339–48.
40. Bhagat S, Arfeen M, Das G, Ramkumar M, Khan SI, Tekwani BL, et al. Design, synthesis and biological evaluation of 4-aminoquinoline-guanylthiourea derivatives as antimalarial agents. Bioorg Chem. 2019 Oct 1; 91:103094.
41.  Hickey J. Anthony. Clinical Trials and Translational Medicine Commentaries Back to the future: Inhaled Drug Products. J Pharm Sci. 2013;102(4):1165–72.

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