Isfahan University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! On (X network) By
Poly(Methyl Vinyl Ether-Co-Maleic Acid) for Enhancement of Solubility, Oral Bioavailability and Anti-Osteoporotic Effects of Raloxifene Hydrochloride Publisher Pubmed



Varshosaz J1 ; Minaiyan M2 ; Dayyani L1
Authors
Show Affiliations
Authors Affiliations
  1. 1. Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Centre, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Pharmacology, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran

Source: European Journal of Pharmaceutical Sciences Published:2018


Abstract

Raloxifene HCl (RH) has poor water solubility and due to its extensive first pass metabolism; its bioavailability is only 2%. The purpose of the present study was to enhance the aqueous solubility, oral bioavailability and anti-osteoporotic effects of RH by electro-sprayed nanoparticles (NPs) in ovariectomized rats. NPs containing RH and different ratio of poly(methyl vinyl ether-co-maleic acid) (PMVEMA) were electrosprayed. The voltage, distance of needle to the collector, flow rate of the solution and polymeric percentage were optimized according to the size of NPs and drug solubility. The optimized formulation was characterized by SEM, XRD, DSC, and FTIR. The pharmacokinetic parameters were studies by oral administration of a single dose of 15 mg/kg in Wistar rats. The anti-osteoporotic effects were studied in female ovariectomized rats. Animals were treated with 6 mg/kg/day for 2 months then serum calcium, phosphorous and alkaline phosphatase levels were measured. RH loaded electrosprayed NPs showed 10-fold enhanced solubility compared to the free drug. Moreover, the XRD and SEM tests displayed an amorphous state of drug in the NPs. FTIR and DSC tests revealed no interaction between the polymer and the drug. Serum calcium, phosphorous and alkaline phosphatase levels were significantly decreased in ovariectomized rats receiving oral RH NPs (P < 0.05). No significant difference was detected between RH NPs and estradiol groups (P > 0.05). Oral bioavailability of NPs showed 7.5-fold increase compared to the pure drug. The electrosprayed PMVEMA nanoparticles can enhance solubility, bioavailability and antiosteoporotic effects of RH. © 2017
Related Docs
View other Related Docs
1. Production of a New Platform Based on Fumed and Mesoporous Silica Nanoparticles for Enhanced Solubility and Oral Bioavailability of Raloxifene Hcl, IET Nanobiotechnology (2019)
2. Enhanced Solubility, Oral Bioavailability and Anti-Osteoporotic Effects of Raloxifene Hcl in Ovariectomized Rats by Igepal Co-890 Nanomicelles, Pharmaceutical Development and Technology (2019)
3. Poly (Butylene Adipate-Co-Butylene Terephthalate) Nanoparticles Prepared by Electrospraying Technique for Docetaxel Delivery in Ovarian Cancer Induced Mice, Drug Development and Industrial Pharmacy (2018)
4. Physicochemical, Pharmacodynamic and Pharmacokinetic Characterization of Soluplus Stabilized Nanosuspension of Tacrolimus, Current Drug Delivery (2017)
5. Fabrication and Characterization of 3D-Printed Composite Scaffolds of Coral-Derived Hydroxyapatite Nanoparticles/Polycaprolactone/Gelatin Carrying Doxorubicin for Bone Tissue Engineering, Journal of Materials Science: Materials in Medicine (2024)
6. Targeted Nanostructured Lipid Carriers for Delivery of Paclitaxel to Cancer Cells: Preparation, Characterization, and Cell Toxicity, Current Drug Delivery (2017)
7. Fabrication of Poly Hydroxybutyrate-Polyethylene Glycol-Folic Acid Nanoparticles Loaded by Paclitaxel, Current Drug Delivery (2016)
8. Development of Lecithin Nanoemulsion Based Organogels for Permeation Enhancement of Metoprolol Through Rat Skin, Journal of Nanomaterials (2013)
Experts (# of related papers)
View all Related Experts
Jaleh Varshosaz (36)
Mohsen Minaiyan (12)
Other Related Docs
9. Transferrin-Targeted Poly(Butylene Adipate)/Terephthalate Nanoparticles for Targeted Delivery of 5-Fluorouracil in Ht29 Colorectal Cancer Cell Line, Journal of Bioactive and Compatible Polymers (2017)
10. Anti-Osteoarthritis Potential of Peppermint and Rosemary Essential Oils in a Nanoemulsion Form: Behavioral, Biochemical, and Histopathological Evidence, BMC Complementary Medicine and Therapies (2021)
11. Preparation and Characterization of Solid Dispersions of Celecoxib Obtained by Spray-Drying Ethanolic Suspensions Containing Pvp-K30 or Isomalt, Journal of Drug Delivery Science and Technology (2018)
12. Plga-Peg-Ra-Based Polymeric Micelles for Tumor Targeted Delivery of Irinotecan, Pharmaceutical Development and Technology (2018)
13. Efavirenz Oral Delivery Via Lipid Nanocapsules: Formulation, Optimisation, and Ex-Vivo Gut Permeation Study, IET Nanobiotechnology (2018)
14. In Vitro Characterisation of a Sol–Gel Derived in Situ Silica-Coated Silicate and Carbonate Co-Doped Hydroxyapatite Nanopowder for Bone Grafting, Materials Science and Engineering C (2017)
15. Poly(Glycerol Sebacate) Nanoparticles for Ocular Delivery of Sunitinib: Physicochemical, Cytotoxic and Allergic Studies, IET Nanobiotechnology (2019)
16. Local Delivery of Usnic Acid Loaded Rhamnolipid Vesicles by Gelatin / Tragacanth Gum / Montmorillonite/ Vanillin Cryogel Scaffold for Expression of Osteogenic Biomarkers and Antimicrobial Activity, Journal of Drug Delivery Science and Technology (2022)
17. Synthesis, Characterization, in Vitro Bioactivity and Biocompatibility Evaluation of Hydroxyapatite/Bredigite (Ca7mgsi4o16) Composite Nanoparticles, JOM (2016)
18. Magnetic Polyvinyl Caprolactam–Polyvinyl Acetate–Polyethylene Glycol Micelles for Docetaxel Delivery in Breast Cancer: An in Vitro Study on Two Cell Lines of Breast Cancer, Pharmaceutical Development and Technology (2017)
19. Development and Optimization of Solid Lipid Nanoparticles of Amikacin by Central Composite Design, Journal of Liposome Research (2010)
20. Preparing Simvastatin Nanoparticles by a Combination of Ph-Sensitive and Timed-Release Approaches for the Potential Treatment of Ulcerative Colitis, Journal of Biomaterials Applications (2022)
21. In Vitro Studies of Polycaprolactone Nanofibrous Scaffolds Containing Novel Gehlenite Nanoparticles, Journal of Medical Signals and Sensors (2021)
22. Design and Optimization of Alginate-Chitosan-Pluronic Nanoparticles As a Novel Meloxicam Drug Delivery System, Journal of Applied Polymer Science (2015)
23. Poly (Ε-Caprolactone) Incorporated Bioactive Glass Nanoparticles and Simvastatin Nanocomposite Nanofibers: Preparation, Characterization and in Vitro Drug Release for Bone Regeneration Applications, Chemical Engineering Journal (2013)
24. Hyaluronate Targeted Solid Lipid Nanoparticles of Etoposide: Optimization and in Vitro Characterization, Journal of Nanomaterials (2014)
25. Poly (Butylene Adipate-Co-Terephthalate) Electrospun Nanofibers Loaded With 5-Fluorouracil and Curcumin in Treatment of Colorectal Cancer Cells, Polymer Testing (2018)
26. Nanocrystalization of Pioglitazone by Precipitation Method, Drug Research (2018)
27. Tissue Distribution and Systemic Toxicity Evaluation of Raloxifene Targeted Polymeric Micelles of Poly (Styrene-Maleic Acid)-Poly (Amide- Ether-Ester-Imide)-Poly (Ethylene Glycol) Loaded With Docetaxel in Breast Cancer Bearing Mice, Recent Patents on Anti-Cancer Drug Discovery (2019)
28. Fabrication and Characterization of Injectable Thermosensitive Hydrogel Containing Dipyridamole Loaded Polycaprolactone Nanoparticles for Bone Tissue Engineering, Journal of Drug Delivery Science and Technology (2021)
29. A Novel Mixed Polymeric Micelle for Co-Delivery of Paclitaxel and Retinoic Acid and Overcoming Multidrug Resistance: Synthesis, Characterization, Cytotoxicity, and Pharmacokinetic Evaluation, Drug Development and Industrial Pharmacy (2018)
30. Effect of Molecular Weight and Molar Ratio of Dextran on Self-Assembly of Dextran Stearate Polymeric Micelles As Nanocarriers for Etoposide, Journal of Nanomaterials (2012)
31. Formulation and Optimization of Solid Lipid Nanoparticles of Buspirone Hcl for Enhancement of Its Oral Bioavailability, Journal of Liposome Research (2010)
32. Effects of Glutaraldehyde and Montmorillonite Percentage on Physicochemical Properties of Agar/Montmorillonite/Xanthan Nano-Composite Scaffolds in Bone Delivery of Alendronate, Journal of Isfahan Medical School (2012)
33. Enhancement of Solubility and Antidiabetic Effects of Repaglinide Using Spray Drying Technique in Stz-Induced Diabetic Rats, Pharmaceutical Development and Technology (2017)
34. Preparation and Characterization of Celecoxib Solid Dispersions; Comparison of Poloxamer-188 and Pvp-K30 As Carriers, Iranian Journal of Basic Medical Sciences (2014)
35. Dual Thermo- and Ph-Responsive Poly(N-Isopropylacrylamide-Co-(2-Dimethylamino) Ethyl Methacrylate)-G-Peg Nanoparticle System and Its Potential in Controlled Drug Release, Polymer Bulletin (2020)
36. Novel Lectin-Modified Poly(Ethylene-Co-Vinyl Acetate) Mucoadhesive Nanoparticles of Carvedilol: Preparation and in Vitro Optimization Using a Two-Level Factorial Design, Pharmaceutical Development and Technology (2014)
37. Optimisation of Processing Variables Effective on Self-Assembly of Folate Targeted Synpronic-Based Micelles for Docetaxel Delivery in Melanoma Cells, IET Nanobiotechnology (2015)
38. Preparation and Characterization of Hydroxyapatite Nanoparticles Doped With Nickel, Tin, and Molybdate Ions for Their Antimicrobial Effects, Drug Development and Industrial Pharmacy (2023)
39. Novel Worm-Like Amphiphilic Micelles of Folate-Targeted Cyclodextrin/Retinoic Acid for Delivery of Doxorubicin in Kg-1 Cells, Colloid and Polymer Science (2014)
40. Electrophoretic-Deposited Hydroxyapatite-Copper Nanocomposite As an Antibacterial Coating for Biomedical Applications, Surface and Coatings Technology (2017)
41. Enhancement of Oral Bioavailability of Pentoxifylline by Solid Lipid Nanoparticles, Journal of Liposome Research (2010)
42. Incorporation of Rosuvastatin-Loaded Chitosan/Chondroitin Sulfate Nanoparticles Into a Thermosensitive Hydrogel for Bone Tissue Engineering: Preparation, Characterization, and Cellular Behavior, Pharmaceutical Development and Technology (2019)
43. Biocompatible Nanocomposite Scaffolds Based on Carrageenan Incorporating Hydroxyapatite and Hesperidin Loaded Nanoparticles for Bone Tissue Regeneration, Polymers for Advanced Technologies (2024)
44. Montelukast Incorporated Poly(Methyl Vinyl Ether-Co-Maleic Acid)/Poly(Lactic-Co-Glycolic Acid) Electrospun Nanofibers for Wound Dressing, Fibers and Polymers (2017)
45. Investigation on Bioactivity and Cytotoxicity of Mesoporous Nano-Composite Mcm-48/Hydroxyapatite for Ibuprofen Drug Delivery, Ceramics International (2014)
46. Preparation and Physicochemical Characterization of Meloxicam Orally Fast Disintegration Tablet Using Its Solid Dispersion, Brazilian Journal of Pharmaceutical Sciences (2017)
47. Production and Evaluation of Polyblend of Agar and Polyacrylonitrile Nanofibers for in Vitro Release of Methotrexate in Cancer Therapy, Fibers and Polymers (2015)
48. Gliclazide Microcrystals Prepared by Two Methods of in Situ Micronization: Pharmacokinetic Studies in Diabetic and Normal Rats, AAPS PharmSciTech (2010)
49. Development and in Vitro/In Vivo Evaluation of a Novel Targeted Polymeric Micelle for Delivery of Paclitaxel, International Journal of Biological Macromolecules (2015)
50. Fabrication and Characterization of a Novel Wound Dressing With Clindamycin Loaded Pva Nanoparticles for Acne Treatment, Fibers and Polymers (2022)