ArticleInternational journal of nanomedicine2018
Design of a transdermal formulation containing raloxifene nanoparticles for osteoporosis treatment.
Article in International journal of nanomedicine, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Who cites it
29 citing papers in PubMed, 51 citations in OpenAlex.
- Nanotechnology-Driven Therapeutic Potential of Raloxifene in Osteoporosis and Cancer: A Recent Review.Current pharmaceutical design · 2026Review
- Pharmacological Behavior of Propylene Glycol/Polyvinyl Alcohol Hydrogel Incorporating Indomethacin Nanocrystals in the Skin.Gels (Basel, Switzerland) · 2025Article
- Nanotechnology in Orthopedic Care: Advances in Drug Delivery, Implants, and Biocompatibility Considerations.International journal of nanomedicine · 2025Review
- Dermal formulation based on carbopol and Gum Arabic improves skin retention of indomethacin.PloS one · 2025Article
- Copolymerized Polymers Based on Cyclodextrins and Cationic Groups Enhance Therapeutic Effect of Rebamipide in the N-Acetylcysteine-Treated Dry Eye Model.Drug design, development and therapy · 2024Article
- An update on the advances in the field of nanostructured drug delivery systems for a variety of orthopedic applications.Drug delivery · 2023Article
- Skin absorption of felbinac solid nanoparticles in gel formulation containing l-menthol and carboxypolymethylene.Journal of pharmaceutical health care and sciences · 2023Article
- Review
- Therapeutic Effects of Hydrogel Formulations Incorporating Troxipide Nanoparticles on Oral Mucositis in Hamsters.Drug design, development and therapy · 2023Article
- Nasal Absorption Enhancement of Mometasone Furoate Nanocrystal Dispersions.International journal of nanomedicine · 2023Article
- QbD-based optimization of raloxifene-loaded cubosomal formulation for transdemal delivery: ex vivo permeability and in vivo pharmacokinetic studies.Drug delivery and translational research · 2022Article
- Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles.Pharmaceutics · 2022Article
- Article
- Minoxidil Nanoparticles Targeting Hair Follicles Enhance Hair Growth in C57BL/6 Mice.Pharmaceutics · 2022Article
- Formulation Development for Transdermal Delivery of Raloxifene, a Chemoprophylactic Agent against Breast Cancer.Pharmaceutics · 2022Article
- Energy-Dependent Endocytosis Is Responsible for Skin Penetration of Formulations Based on a Combination of Indomethacin Nanoparticles and l-Menthol in Rat and Göttingen Minipig.International journal of molecular sciences · 2021Article
- Transdermal System Based on Solid Cilostazol Nanoparticles Attenuates Ischemia/Reperfusion-Induced Brain Injury in Mice.Nanomaterials (Basel, Switzerland) · 2021Article
- Nanotechnology-based drug delivery systems in orthopedics.Joint diseases and related surgery · 2021Review
- Hydrogel Formulations Incorporating Drug Nanocrystals Enhance the Therapeutic Effect of Rebamipide in a Hamster Model for Oral Mucositis.Pharmaceutics · 2020Article
- Development of Sustained-Release Ophthalmic Formulation Based on Tranilast Solid Nanoparticles.Materials (Basel, Switzerland) · 2020Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeIn the clinical setting, raloxifene, a second-generation selective estrogen receptor modulator, is administered orally; however, the bioavailability (BA) is only 2% because of its poor solubility in aqueous fluids and its extensive first-pass metabolism. Therefore, it is expected that the development of a transdermally delivered formulation may reduce the necessary dose without compromising its therapeutic efficacy. In this study, we designed transdermal formulations containing raloxifene nanoparticles and evaluated their usefulness for osteoporosis therapy.
methodsRaloxifene was crushed with methylcellulose by the bead mill method, and the milled raloxifene was gelled with or without menthol (a permeation enhancer) by Carbopol
resultsThe mean particle size of raloxifene in the transdermal formulation (Ral-NPs) was 173.7 nm. Although the raloxifene released from Ral-NPs remained in the nanoparticle state, the skin penetration of raloxifene nanoparticles was prevented by the stratum corneum in rat. On the other hand, inclusion of menthol in the formulation attenuated the barrier function of the stratum corneum and permitted the penetration of raloxifene nanoparticles through the skin. Moreover, macropinocytosis relates to the skin penetration of the formulation including menthol (mRal-NPs), since penetration was inhibited by treatment with 2 µM rottlerin, a macropinocytosis inhibitor. In addition, the application of 0.3% mRal-NPs (once a day) attenuated the decreases in calcium level and stiffness of the bones of ovariectomized rat.
conclusionWe prepared raloxifene solid nanoparticles by a bead mill method and designed a novel transdermal formulation containing nanoparticles and permeation enhancers. These trans-dermal formulations overcome the barrier properties of the skin and show high drug penetration through the transdermal route (BA 8.5%). In addition, we found that raloxifene transdermal formulations are useful for the treatment of osteoporosis in ovariectomized rat.
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