Raloxifene encapsulated spanlastic nanogel for the prevention of bone fracture risk via transdermal administration : Pharmacokinetic and efficacy study in animal model
© 2023. Controlled Release Society..
This research work is to evaluate spanlastic-loaded raloxifene (RLX) nanogel administration via the transdermal route to avoid its hepatic metabolism and to enhance the bioavailability for better management of osteoporosis. RLX-loaded spanlastic nanogel was prepared and characterized for its viscosity, pH, spreadability, and texture profile. The formulation was applied on the skin surface of the animal for pharmacokinetic evaluation, and later, the efficacy of the formulation was assessed in ovariectomized female Wistar rats. The nanogel was obtained with a viscosity (2552.66 ± 30.61 cP), pH (7.1 ± 0.1), and spreadability (7.1 ± 0.2 cm). The texture properties, cohesiveness, and adhesiveness of the nanogel showed its suitability for transdermal application. Nanogel showed no sign of edema and erythema in the skin irritation test which revealed its safety for transdermal application. The t1/2 obtained for RLX-spanlastic nanogel (37.02 ± 0.59 h) was much higher than that obtained for RLX-oral suspension (14.43 h). The relative bioavailability was found to be 215.96% for RLX-spanlastic nanogel, and the drug and formulation did not show any toxicity in any of the vital organs, as well as no hematological changes occurring in blood samples. In microarchitectural measurement, RLX-spanlastic nanogel exhibited no unambiguous deviations along with improved bone mineral density compared to the RLX suspension treated group. Transdermal administration of RLX-spanlastic nanogel showed significant improvement of drug bioavailability (approx. twice to oral administration) without any toxic effect in the treated rats. Hence, spanlastic nanogel could be a better approach to deliver RLX via transdermal route for the management of osteoporosis.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2024 |
|---|---|
| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
|---|---|
| Enthalten in: |
Drug delivery and translational research - 14(2024), 6 vom: 01. Apr., Seite 1635-1647 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Ansari, Mohd Danish [VerfasserIn] |
|---|
| Links: |
|---|
| Anmerkungen: |
Date Completed 26.04.2024 Date Revised 26.04.2024 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.1007/s13346-023-01480-y |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM364879823 |
|---|
| LEADER | 01000caa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM364879823 | ||
| 003 | DE-627 | ||
| 005 | 20240427232013.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231226s2024 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1007/s13346-023-01480-y |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1390.xml |
| 035 | |a (DE-627)NLM364879823 | ||
| 035 | |a (NLM)37996726 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Ansari, Mohd Danish |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Raloxifene encapsulated spanlastic nanogel for the prevention of bone fracture risk via transdermal administration |b Pharmacokinetic and efficacy study in animal model |
| 264 | 1 | |c 2024 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 26.04.2024 | ||
| 500 | |a Date Revised 26.04.2024 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2023. Controlled Release Society. | ||
| 520 | |a This research work is to evaluate spanlastic-loaded raloxifene (RLX) nanogel administration via the transdermal route to avoid its hepatic metabolism and to enhance the bioavailability for better management of osteoporosis. RLX-loaded spanlastic nanogel was prepared and characterized for its viscosity, pH, spreadability, and texture profile. The formulation was applied on the skin surface of the animal for pharmacokinetic evaluation, and later, the efficacy of the formulation was assessed in ovariectomized female Wistar rats. The nanogel was obtained with a viscosity (2552.66 ± 30.61 cP), pH (7.1 ± 0.1), and spreadability (7.1 ± 0.2 cm). The texture properties, cohesiveness, and adhesiveness of the nanogel showed its suitability for transdermal application. Nanogel showed no sign of edema and erythema in the skin irritation test which revealed its safety for transdermal application. The t1/2 obtained for RLX-spanlastic nanogel (37.02 ± 0.59 h) was much higher than that obtained for RLX-oral suspension (14.43 h). The relative bioavailability was found to be 215.96% for RLX-spanlastic nanogel, and the drug and formulation did not show any toxicity in any of the vital organs, as well as no hematological changes occurring in blood samples. In microarchitectural measurement, RLX-spanlastic nanogel exhibited no unambiguous deviations along with improved bone mineral density compared to the RLX suspension treated group. Transdermal administration of RLX-spanlastic nanogel showed significant improvement of drug bioavailability (approx. twice to oral administration) without any toxic effect in the treated rats. Hence, spanlastic nanogel could be a better approach to deliver RLX via transdermal route for the management of osteoporosis | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Histopathology study | |
| 650 | 4 | |a Micro-CT | |
| 650 | 4 | |a Raloxifene (RLX) HCL | |
| 650 | 4 | |a Spanlastic nanogel | |
| 650 | 4 | |a Transdermal delivery | |
| 650 | 7 | |a Raloxifene Hydrochloride |2 NLM | |
| 650 | 7 | |a 4F86W47BR6 |2 NLM | |
| 650 | 7 | |a Bone Density Conservation Agents |2 NLM | |
| 650 | 7 | |a Nanogels |2 NLM | |
| 650 | 7 | |a Drug Carriers |2 NLM | |
| 650 | 7 | |a Polyethylene Glycols |2 NLM | |
| 650 | 7 | |a 3WJQ0SDW1A |2 NLM | |
| 700 | 1 | |a Shafi, Sadat |e verfasserin |4 aut | |
| 700 | 1 | |a Pandit, Jayamanti |e verfasserin |4 aut | |
| 700 | 1 | |a Waheed, Ayesha |e verfasserin |4 aut | |
| 700 | 1 | |a Jahan, Rao Nargis |e verfasserin |4 aut | |
| 700 | 1 | |a Khan, Iram |e verfasserin |4 aut | |
| 700 | 1 | |a Vohora, Divya |e verfasserin |4 aut | |
| 700 | 1 | |a Jain, Shreshta |e verfasserin |4 aut | |
| 700 | 1 | |a Aqil, Mohd |e verfasserin |4 aut | |
| 700 | 1 | |a Sultana, Yasmin |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Drug delivery and translational research |d 2011 |g 14(2024), 6 vom: 01. Apr., Seite 1635-1647 |w (DE-627)NLM207177104 |x 2190-3948 |7 nnns |
| 773 | 1 | 8 | |g volume:14 |g year:2024 |g number:6 |g day:01 |g month:04 |g pages:1635-1647 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.1007/s13346-023-01480-y |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 14 |j 2024 |e 6 |b 01 |c 04 |h 1635-1647 | ||