Solubility enhancement of meloxicam by phospholipid complexation

  • Vaibhav Bhadange Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India
  • Pravin Kawtikwar Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India
  • Supriya Jogdand Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India
  • Ankita Kawtikwar Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Abstract

The best solubility enhancement approach is phospholipids complexation. It has been effectively employed by a number of writers to enhance the permeability, oral bioavailability, and solubility of several medicinal substances. The meloxicam is a member of BCS Class II, and because of its poor solubility and high permeability, its clinical application may have been constrained. Therefore, it is necessary to use a method that modifies the biopharmaceutical features. In this work, meloxicam, an NSAID with demonstrated anticancer action, was combined with phospholipid to increase its solubility. Utilizing solvent evaporation, the meloxicam phospholipid complex was produced. Particle size, zeta potential, SEM analysis, in vitro drug release, and solubility were assessed for the produced complex. The results obtained in this study showed the smaller particle size in nanometer range and physical stability with desired zeta potential. Meloxicam's prolonged release from the phospholipid complex is demonstrated by the in vitro drug release investigation.  The apparent solubility analysis of meloxicam phospholipid complex. Pure meloxicam showed that the drug's solubility was several times higher than that of the pure form. Hence in conclusion we can say that the phospholipid complexation could be the ideal method for solubility enhancement of drug like meloxicam.


Keyword: Meloxicam, phospholipid complex, solubility, drug release

Keywords: Meloxicam, phospholipid complex, solubility, drug release

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Author Biographies

Vaibhav Bhadange, Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Pravin Kawtikwar, Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Supriya Jogdand, Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Ankita Kawtikwar, Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

Sudhakarao Naik College of Pharmacy, Nagpur Road, Pusad- 445 204, Dist.- Yavatmal, Maharashtra, India

References

1. Rarokar N, Gurav S, Khedekar P. Meloxicam encapsulated nanostructured colloidal self‐assembly for evaluating antitumor and anti‐inflammatory efficacy in 3D printed scaffolds. Journal of Biomedical Materials Research Part A. 2021 Aug;109(8):1441-56. https://doi.org/10.1002/jbm.a.37135 PMid:33289225
2. Abdulateef SA, Hussein MH, Al-Saffar AZ. In vitro cytotoxic and genotoxic of lipopolysaccharide isolated from klebsiella pneumoniae as1 on mcf-7 human breast tumor cell line. International Journal of. Drug Delivery Technology. 2021;11(1):184-9.
3. Bolourchian N, Nili M, Shahhosseini S, Nokhodchi A, Foroutan SM. Crystallization of meloxicam in the presence of hydrophilic additives to tailor its physicochemical and pharmaceutical properties. Journal of Drug Delivery Science and Technology. 2021 Dec 1;66:102926. https://doi.org/10.1016/j.jddst.2021.102926
4. Bhange M and Jadhav A. Formulation and Development of Novel Matrix Dispersion System based on Phospholipid Complex for Improving Oral Bioavailability of Ferulic Acid. International Journal of Drug Delivery and Technology. 2022;12(4):1489-1495. https://doi.org/10.25258/ijddt.12.4.01
5. Saoji SD, Raut NA, Dhore PW, Borkar CD, Popielarczyk M, Dave VS. Preparation and evaluation of phospholipid-based complex of standardized centella extract (SCE) for the enhanced delivery of phytoconstituents. The AAPS journal. 2016 Jan;18:102-14. https://doi.org/10.1208/s12248-015-9837-2 PMid:26563253 PMCid:PMC7583548
6. Telange DR, Patil AT, Pethe AM, Fegade H, Anand S, Dave VS. Formulation and characterization of an apigenin-phospholipid phytosome (APLC) for improved solubility, in vivo bioavailability, and antioxidant potential. European Journal of Pharmaceutical Sciences. 2017 Oct 15;108:36-49. https://doi.org/10.1016/j.ejps.2016.12.009 PMid:27939619
7. Rarokar NR, Telange DR, Kalsait RP, Khedekar PB. Solubility enhancement of extract of Lagenariasiceraria by development of Phospholipon® 90 H modulated phospholipid complex employing Box-Behnken design. In Annales Pharmaceutiques Françaises 2022 Nov 11. Elsevier Masson. https://doi.org/10.1016/j.pharma.2022.11.007 PMid:36375530
8. Saoji SD, Rarokar NR, Dhore PW, Dube SO, Gurav NS, Gurav SS, Raut NA. Phospholipid based colloidal nanocarriers for enhanced solubility and therapeutic efficacy of withanolides. Journal of Drug Delivery Science and Technology. 2022 Apr 1;70:103251. https://doi.org/10.1016/j.jddst.2022.103251
9. Zhang Z, Lin Y, Liu F. Preparation and characterization of CdS/ZnS core-shell nanoparticles. Journal of Dispersion Science and Technology. 2020 Apr 15;41(5):725-32. https://doi.org/10.1080/01932691.2019.1611441
10. Rarokar NR, Saoji SD, Raut NA, Taksande JB, Khedekar PB, Dave VS. Nanostructured cubosomes in a thermoresponsive depot system: an alternative approach for the controlled delivery of docetaxel. AAPS PharmSciTech. 2016 Apr;17:436-45. https://doi.org/10.1208/s12249-015-0369-y PMid:26208439 PMCid:PMC4984890
11. Paruchuri VK, Nguyen AV, Miller JD. Zeta-potentials of self-assembled surface micelles of ionic surfactants adsorbed at hydrophobic graphite surfaces. Colloids and Surfaces A: Physicochemical and Engineering Aspects. 2004 Dec 10;250(1-3):519-26. https://doi.org/10.1016/j.colsurfa.2004.04.098
12. Rarokar N, Agrawal R, Yadav S, Khedekar P, Ravikumar C, Telange D, Gurav S. Pteroyl-γ-l-glutamate/Pluronic® F68 modified polymeric micelles loaded with docetaxel for targeted delivery and reduced toxicity. Journal of Molecular Liquids. 2023 Jan 1;369:120842. https://doi.org/10.1016/j.molliq.2022.120842
13. Zeng X, Tao W, Mei L, Huang L, Tan C, Feng SS. Cholic acid-functionalized nanoparticles of star-shaped PLGA-vitamin E TPGS copolymer for docetaxel delivery to cervical cancer. Biomaterials. 2013 Aug 1;34(25):6058-67. https://doi.org/10.1016/j.biomaterials.2013.04.052 PMid:23694904
14. Rodrigues K, Nadaf S, Rarokar N, Gurav N, Jagtap P, Mali P, Ayyanar M, Kalaskar M, Gurav S. QBD approach for the development of hesperetin loaded colloidal nanosponges for sustained delivery: In-vitro, ex-vivo, and in-vivo assessment. OpenNano. 2022 Jul 1;7:100045. https://doi.org/10.1016/j.onano.2022.100045
15. Wang H, Li Q, Reyes S, Zhang J, Xie L, Melendez V, Hickman M, Kozar MP. Formulation and particle size reduction improve bioavailability of poorly water-soluble compounds with antimalarial activity. Malaria Research and Treatment. 2013;2013. https://doi.org/10.1155/2013/769234 PMid:23766925 PMCid:PMC3666196
16. Freitas C, Müller RH. Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN™) dispersions. International journal of pharmaceutics. 1998 Jun 15;168(2):221-9. https://doi.org/10.1016/S0378-5173(98)00092-1
17. Elnakat H. Distribution, functionality and gene regulation of folate receptor isoforms: implications in targeted therapy. Advanced drug delivery reviews. 2004 Apr 29;56(8):1067-84. https://doi.org/10.1016/j.addr.2004.01.001 PMid:15094207
18. O'Shannessy DJ, Somers EB, Palmer LM, Thiel RP, Oberoi P, Heath R, Marcucci L. Serum folate receptor alpha, mesothelin and megakaryocyte potentiating factor in ovarian cancer: association to disease stage and grade and comparison to CA125 and HE4. Journal of ovarian research. 2013 Dec;6(1):1-6. https://doi.org/10.1186/1757-2215-6-29 PMid:23590973 PMCid:PMC3640997
19. Allard JE, Risinger JI, Morrison C, Young G, Rose GS, Fowler J, Berchuck A, Maxwell GL. Overexpression of folate binding protein is associated with shortened progression-free survival in uterine adenocarcinomas. Gynecologic oncology. 2007 Oct 1;107(1):52-7. https://doi.org/10.1016/j.ygyno.2007.05.018 PMid:17582475
20. Rarokar NR, Khedekar PB, Bharne AP, Umekar MJ. Development of self-assembled nanocarriers to enhance antitumor efficacy of docetaxeltrihydrate in MDA-MB-231 cell line. International journal of biological macromolecules. 2019 Mar 15;125:1056-68. https://doi.org/10.1016/j.ijbiomac.2018.12.130 PMid:30572051
21. Xu Z, Liu S, Kang Y, Wang M. Glutathione-responsive polymeric micelles formed by a biodegradable amphiphilic triblock copolymer for anticancer drug delivery and controlled release. ACS Biomaterials Science & Engineering. 2015 Jul 13;1(7):585-92. https://doi.org/10.1021/acsbiomaterials.5b00119 PMid:33434974
22. Weyna DR, Cheney ML, Shan N, Hanna M, Zaworotko MJ, Sava V, Song S, Sanchez-Ramos JR. Improving solubility and pharmacokinetics of meloxicam via multiple-component crystal formation. Molecular pharmaceutics. 2012 Jul 2;9(7):2094-102. https://doi.org/10.1021/mp300169c PMid:22642304
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1.
Bhadange V, Kawtikwar P, Jogdand S, Kawtikwar A. Solubility enhancement of meloxicam by phospholipid complexation. JDDT [Internet]. 15Jan.2024 [cited 25Feb.2024];14(1):91-5. Available from: https://jddtonline.info/index.php/jddt/article/view/6390