FORMULATION AND EVALUATION OF OPTIMISED MALTODEXTRIN BASED PRONIOSOME POWDERS CONTAINING BAZEDOXIFENE ACETATE FOR ORAL DELIVERY
DOI:
https://doi.org/10.22159/ijcpr.2020v12i6.40285Keywords:
Proniosomes, Niosomes, Permeability, Pharmacokinetics, BioavailabilityAbstract
Objective: The main objective of the present study was to develop proniosomal formulations to enhance the oral bioavailability of bazedoxifene acetate by improving solubility, dissolution and/or intestinal permeability.
Methods: Proniosomal powder formulations were prepared with bazedoxifene acetate drug varying the span 40 and cholesterol ratio in the range of 0.8:0.2 to 0.2:0.8 using maltodextrin as a carrier by slurry method. The prepared proniosomal powder was filled into capsules. The bioavailability enhancement of proniosomes loaded with drug was studied focusing on non-ionic surfactants composition and drug: span 40 ratio. Prepared proniosomes were characterized for their particle size distribution, zeta potential, entrapment efficiency, in vitro dissolution study and thermal characteristics to understand the phase transition behavior. Further, the formulated proniosomes were subjected to stability behavior, ex vivo permeation studies using rat intestine followed by in vivo studies.
Results: Physico-chemical studies help in the optimization of formulations. Enhancement in dissolution is due to the incorporation of bazedoxifene acetate into the non-ionic surfactant and change in the physical state from crystalline to amorphous, thus improving oral bioavailability. Ex vivo studies show significant permeation enhancement across the gastrointestinal membrane compared to control.
Conclusion: In conclusion, proniosomes provide a powerful and functional way of the distribution of inadequately soluble bazedoxifene acetate drug, which is proved from in vivo studies based on the enhanced oral delivery.
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References
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33. Blazek Welsh AI, Rhodes DG. SEM imaging predicts quality of niosomes from maltodextrin-based proniosomes. Pharm Res 2001;18:656–61.
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35. Pradip KG, Rita JM, Manish LU, Rayasa SRM. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSciTech 2006;7:E1–E5.
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38. Almira I Blamek Welsh, David G Rhodes. Maltodextrin–based proniosomes. Pharm Sci 2001;3:1-8.
39. Gupta A, Prajapati SK, Singh M, Balamurugan M. Proniosomal powder of captopril: formulation and evaluation. Mol Pharm 2007;4:596-9.
40. Solanki AB, Parikh JR, Parikh RH. Formulation and optimization of piroxicam proniosomes by 3-factor, 3-level box-behnken design. AAPS PharmSciTech 2007;8:E1–E7.
41. Plessis J, Ramachandran C, Weiner N, Miller DG. The influence of particle size of liposomes on deposition of drug into skin. Int J Pharm 1991;103:277–82.
42. Namdeo A, Jain NK. Niosomal delivery of 5-fluorouracil. J Microencapsul 1999;16:731–40.
43. Uchegbu IF, Florence AT. Non-ionic surfactant vesicles (niosomes): physical and pharmaceutical chemistry. Adv Coll Interf Sci 1995;58:1-55.
44. Praveen SH, Kumaresh SS, Guru VB. Proliposomes of exemestane for improved oral delivery: formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine. Int J Pharm 2009;380:96-104.
45. Bradbury S, Joy DC, Ford BJ. Transmission electron microscope (TEM). Encyclopedia Britannica; 2011.
46. Cornaire G, Woodley J, Hermann P, Cloarec A, Arellano C, Houin G. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int J Pharm 2004;278:119–31.
2. Smitha G, Areefulla SH, Swamy PV. Enhancement of in vitro dissolution characteristics of nifedipine by co-grinding technique. Int J Pharm Chem Sci 2012;1:1279-85.
3. Mullins JD, Macek TJ. Some pharmaceutical properties of novobiocin. J Am Pharm Assoc 1960;49:245-8.
4. Atkinson RM, Bedford C, Child KJ, Tomich EG. Effect of particle size on blood griseofulvin-levels in man. Nature 1962;193:588-9.
5. O’Driscoll CM, Griffin BT. Biopharmaceutical challenges associated with drugs with low aqueous solubility–the potential impact of lipid-based formulations. Adv Drug Delivery Rev 2008;60:617–24.
6. Tang B, Cheng G, Gu JC, Xu CH. Development of solid self-emulsifying drug delivery systems: preparation techniques and dosage forms. Drug Discovery Today 2008;13:606–12.
7. Jha AK, Kumar R, Kumar S, Jha SS. Vesicular system carrier for drug delivery. Der Pharm Sin 2011;2:192-202.
8. Schreier H, Bouwstra J. Liposomes and niosomes as topical drug carriers: dermal and transdermal drug delivery. J Controlled Release 1994;30:1–15.
9. Ijeoma FU, Vyas SP. Non-ionic surfactant based vesicles (niosomes) in drug delivery. Int J Pharm 1998;172:33–70.
10. Deepthi Annakula, Madhukar Rao Errabelli, Raju Jukanti, Suresh Bandari, Prabhakar Reddy Veerareddy. Provesicular drug delivery systems: an overview and appraisal. Arch Appl Sci Res 2010;2:135-46.
11. Sarala Y, Natarajan V, Veeran GK, Zhijun W, Manish I, Guru VB. Proliposomes as a drug delivery system to decrease the hepatic first-pass metabolism: case study using a model drug. Eur J Pharm Sci 2014;64:26–36.
12. Yasam VR, Jakki SL, Natarajan J, Kuppusamy G. A review on novel vesicular drug delivery: proniosomes. Drug Delivery 2014;21:243-9.
13. Gangadharappa HV, Gangadhar V, Nagashubha B. Approaches for improvement of vesicular system-pro-vesicular drug delivery. Am J Pharm Tech Res 2014;4:16-57.
14. Bayindir ZS, Yuksel N. Provesicles as novel drug delivery systems. Curr Pharm Biotechnol 2015;16:344-64.
15. Hu C, Rhodes DG. Proniosomes: a novel drug carrier preparation. Int J Pharm 1999;185:23-35.
16. Gannu PK, Pogaku R. Nonionic surfactant vesicular systems for effective drug delivery-an overview. Acta Pharm Sinica B 2011;1:208-19.
17. Abd-Elbary A, El-laithy HM, Tadros MI. Sucrose stearate-based proniosome-derived niosomes for the nebulisable delivery of cromolyn sodium. Int J Pharm 2008;357:189–98.
18. Sankar V, Ruckmani K, Durga S, Jailani S. Proniosomes as drug carriers. Pak J Pharm Sci 2010;23:103-7.
19. Akhilesh D, Hazel G, Kamath JV. Proniosomes–a propitious Provesecular drug carrier. Int J Pharm Pharm Sci Res 2011;1:98-103.
20. Jaime Kulak Junior, Carolina Aguiar Moreira Kulak, Hugh S Taylor. SERMs in the prevention and treatment of postmenopausal osteoporosis: an update. Arq Bras Endocrinol Metabol 2010;54:200–5.
21. Hadji P. The evolution of selective estrogen receptor modulators in osteoporosis therapy. Climacteric 2012;15:513–23.
22. Chines AA, Komm BS. Bazedoxifene acetate: a novel selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis. Drugs Today (Barc) 2009;45:507-20.
23. Diana MS, Stefanie CN. Bazedoxifene: an investigational selective estrogen receptor modulator for the treatment and prevention of osteoporosis in postmenopausal women. Formulary 2011;46:159-76.
24. Ronkin S, Northington R, Baracat E, Nunes MG, Archer DF, Constantine G, et al. Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol 2005;105:1397–404.
25. Nagasamy Venkatesh D, Swetha Priyanka V, Tulasi K, Kalyani K, Sheik Abid Ali, Harikrishna J. Proniosomes: a superior drug delivery system. Int J Pharm Sci Drug Res 2014;6:178-82.
26. Bangham AD, Standish MM, Watkins JC. Diffusion of univalent ions across the lamellae of swollen phospholipids. J Mol Biol 1965;13:238–52.
27. Staniforth J. Powder flow. In: M Aulton. ed. Pharmaceutics, The Science of Dosage form Design. second ed. Churchill Livingstone: Longman Group Edinburgh; 2002. p. 197–210.
28. Lieberman HA, Lachman L, Schwartz JB. Pharmaceutical dosage forms: Tablets, Marcel Dekker, New York; 1990. p. 201-43.
29. Carr RL. Evaluation of flow properties of solids. Chem Eng 1965;72:163–8.
30. Manjunath K, Venkateswarlu V. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J Controlled Release 2005;107:215–28.
31. Jukanti R, Sheela S, Bandari S, Veerareddy PR. Enhanced bioavailability of exemestane via proliposomes based transdermal delivery. J Pharm Sci 2011;100:3208–22.
32. Smitha G. Determination of bazedoxifene acetate in bulk with the aid of Uv-spectroscopy: development and validation. Int J Pharm Tech Res 2014;7:641-7.
33. Blazek Welsh AI, Rhodes DG. SEM imaging predicts quality of niosomes from maltodextrin-based proniosomes. Pharm Res 2001;18:656–61.
34. Mohamed S El-Ridy, Alia A Badawi, Marwa M Safar, Amira M Mohsen. Niosomes as a novel pharmaceutical formulation encapsulating the hepatoprotective drug silymarin. Int J Pharm Pharm Sci 2012;4:549-59.
35. Pradip KG, Rita JM, Manish LU, Rayasa SRM. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSciTech 2006;7:E1–E5.
36. Gandra S, Sheelam SCR, Maddela R, Reddymalla P, Bakshi V, Jukanti R. Bazedoxifene acetate quantification in rat serum with the aid of RP-HPLC: method development and validation. World J Pharm Sci 2015;3:2357-63.
37. Nel I, Gauler TC, Eberhardt WE, Nickel AC, Schuler M, Thomale J, et al. Formation and repair kinetics of Pt-(GpG) DNA adducts in extracted circulating tumour cells and response to platinum treatment. Br J Cancer 2013;109:1223–9.
38. Almira I Blamek Welsh, David G Rhodes. Maltodextrin–based proniosomes. Pharm Sci 2001;3:1-8.
39. Gupta A, Prajapati SK, Singh M, Balamurugan M. Proniosomal powder of captopril: formulation and evaluation. Mol Pharm 2007;4:596-9.
40. Solanki AB, Parikh JR, Parikh RH. Formulation and optimization of piroxicam proniosomes by 3-factor, 3-level box-behnken design. AAPS PharmSciTech 2007;8:E1–E7.
41. Plessis J, Ramachandran C, Weiner N, Miller DG. The influence of particle size of liposomes on deposition of drug into skin. Int J Pharm 1991;103:277–82.
42. Namdeo A, Jain NK. Niosomal delivery of 5-fluorouracil. J Microencapsul 1999;16:731–40.
43. Uchegbu IF, Florence AT. Non-ionic surfactant vesicles (niosomes): physical and pharmaceutical chemistry. Adv Coll Interf Sci 1995;58:1-55.
44. Praveen SH, Kumaresh SS, Guru VB. Proliposomes of exemestane for improved oral delivery: formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine. Int J Pharm 2009;380:96-104.
45. Bradbury S, Joy DC, Ford BJ. Transmission electron microscope (TEM). Encyclopedia Britannica; 2011.
46. Cornaire G, Woodley J, Hermann P, Cloarec A, Arellano C, Houin G. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int J Pharm 2004;278:119–31.
Published
15-11-2020
How to Cite
GANDRA, S. “FORMULATION AND EVALUATION OF OPTIMISED MALTODEXTRIN BASED PRONIOSOME POWDERS CONTAINING BAZEDOXIFENE ACETATE FOR ORAL DELIVERY”. International Journal of Current Pharmaceutical Research, vol. 12, no. 6, Nov. 2020, pp. 56-66, doi:10.22159/ijcpr.2020v12i6.40285.
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