Volume : 12, Issue : 02, February – 2025
Title:
FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF RALOXIFENE FOR IMPROVING BIOAVAILABILITY
Authors :
Cheekati Reshma, Pasham Venkanna*
Abstract :
Raloxifene hydrochloride (RLX) is a selective estrogen receptor modulator with poor bioavailability of 2% and extensive first-pass metabolism. They have been developed to treat postmenopausal osteoporosis to improve the oral bioavailability of raloxifene-loaded solid lipid nanoparticles (RLX-SLNs). The RLX-SLNs were produced using hot homogenization followed by an ultrasonication technique. The developed RLX-SLNs have shown the mean size of particles is 244-310 nm, and Zeta potential (ZP) values varied from -20.4 ± 0.59 to -39.8 ± 1.89 mV, indicating the stability of fabricated RLX-SLNs. The entrapment efficiency (EE) was between 74% and 82%. The pharmacokinetic studies were conducted on Wistar rats, the optimized formulations of RLX 5, and the coarse suspension of pure drug administered orally. The optimized formulation has bioavailability was increased 1.71 folds and differentiated with the coarse suspension.
Keywords: Bioavailability, solid lipid nanoparticles, raloxifene, homogenization and ultrasonication.
Cite This Article:
Please cite this article in press Cheekati Reshma et al.,Formulation And Evaluation Of Solid Lipid Nanoparticles Of Raloxifene For Improving Bioavailability.,Indo Am. J. P. Sci, 2025; 12 (02).
Number of Downloads : 10
References:
1. Mukherjee S, Ray S, Thakur RS. Solid lipid nanoparticles: A modern formulation approach in drug delivery system. Indian J Pharm Sci. 2009; 71:349–58.
2. Delie F, Blanco-Príeto MJ. Polymeric particulates to improve oral bioavailability of peptide drugs. Molecules. 2005; 10:65–80.
3. Akanksha Garud, Deepti Singh, Navneet Garud. Solid Lipid Nanoparticles (SLN): Method, Characterization and Applications. International Current Pharmaceutical Journal 2012; 1(11):384- 393.
4. Jana Pardeike, Aiman Hommoss, Rainer H Muller. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. International Journal of Pharmaceutics 2009;366(1-2):170-184.
5. R H Muller, M. Radtke, S A Wissing. Nanostructured lipid matrices for improved microencapsulation of drugs. International Journal of Pharmaceutics 2002;(1-2):121-128.
6. Ekambaram P, Sathali AA. Formulation and evaluation of solid lipid nanoparticles of ramipril. J Young Pharmacists 2011; 3(3):216-220.
7. Melike Uner, Gulgun Yene. Importance of solid lipid nanoparticles in various administration routes and future perspectives. International Journal of Nanomedicine 2007;2(3):289-300.
8. JS Mulla, IM Khazi, Naveen Kumar Sharma, SP Hiremath, VG Jamakandi. Solid lipid nanoparticles: methods of preparation. Indian Journal of Novel Drug Delivery 2011;3(3): 170-175.
9. W Mehnert, K Madr. Solid lipid nanoparticles: production, characterization and applications. Advanced Drug Delivery Reviews 2001;47(2-3):165–196.
10. Hu FQ, Yuan H, Zhang HH, Fang M. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. International Journal of Pharmaceutics 2002;239(1-2):121-128.
11. Harshad Harde, Manasmita Das, Sanyog Jain. Solid lipid nanoparticles: An oral bioavailability enhancer vehicle. Expert onion drug delivery 2011;8(11):1407-1424. Daniela Chirio, Marina Gallarate, Elena Peira, Luigi Battaglia, Loredana Serpe and Michele Trotta. Formulation of curcumin-loaded solid lipid nanoparticles produced by fatty acids coacervation technique. Journal of Microencapsulation 2011; 28(6): 537-548.
12. Olbrich, Oliver Kayser and Rainer Helmut Muller. Enzymatic degradation of Dynasan 114 SLN effect of surfactants and particle size. Journal of Nanoparticle Technology and Applications Research 2002;4(1):121–129.
13. Arjun Narala and Kishan Veerabrahma. Preparation, characterization and evaluation of quetiapine fumarate solid lipid nanoparticles to improve oral bioavailability. Journal of Pharmaceutics 2013; 1-7.
14. Shuyu Xie, Luyan Zhu, Zhao Dong, Yan Wang, Xiaofang Wang, and WenZhong Zhou. Preparation and evaluation of ofloxacin-loaded palmitic acid solid lipid nanoparticles. International Journal of Nanomedicine 2011;6: 547–555.
15. Marcos Garcia Fuentes, Dolores Torres, Maria Jose Alonso. New surface-modified lipid nanoparticles as delivery vehicles for salmon calcitonin. International Journal of Pharmaceutics 2005; 296:122-132.
16. L. Hu, Q. Xing, J. Meng, and C. Shang. Preparation and enhanced oral bioavailability of cryptotanshinone-loaded solid lipid nanoparticles. AAPS PharmSciTech 2010;11(2):582- 587.
17. Shagufta Khan Tripti Tiwari, Shweta Tyagi, Mithun Bhowmik, Amit Joshi, Balkrishna Dubey. Preformulation studies and preparation of dithranol-loaded solid lipid nanoparticles. International journal of research and development in pharmacy and life sciences 2012;1(4):183-188.
18. G Suresh, K Manjunath, Vobalaboina Venkateswarlu and V Satyanarayana. Preparation, characterization, and in vitro and in vivo evaluation of lovastatin solid lipid nanoparticles.
AAPS PharmSciTech, 2007;8(1):162-170.
19. Jawahar N, Eaggapanath T, Nagaswamy V, Samantha JS. Preparation and characterization of PLGA nanoparticles containing a hypertensive agent. Int J Pharm Tech Res 2009; 2:390-393.
20. Yang SC, LU LF. Cai Y. Body distribution in mice of intravenously injected camptothecin solid lipid nanoparticles and targeting effect on brain. J. Control. Release, 1999; 2; 59(3).299-307.




