Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization

Mahmut Ozan Toksoy

Article Details

Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization

Authors:

Mahmut Ozan Toksoy

Publisher:

Marmara University

Main Topics:

Pharmaceutical Delivery Technologies

Journal:

Journal of Research in Pharmacy Vol.25 Issue 5, pp.702-714

Document Type:

Article

Publication Date:

6/2025

Document Language:

English

Document ID (Org No.):

2001346236

pISSN:

2630-6344

Keywords:

Abstract:

 Rasagiline mesylate RM is a selective irreversible MAO-B inhibitor used in the treatment of Parkinsons disease. This study was designed to prepare and optimize RM loaded solid lipid nanoparticles RM-SLNs in a thermosensitive mucoadhesive gel RM-SLNs-GEL. RM-SLNs were prepared combining Gelucire 5013 10, Labrasol 0.3 Cremophor RH40 12 with a mixing rate and time of 500 rpm, 45 min. Mucoadhesive gels were prepared combining Poloxamer 407 and HPMC E5 15.5  0.25. Optimized formulation RM-SLNs-GEL was evaluated for sol-gel transition temperature, viscosity, mucoadhesive force, particle size and distribution, SEM imaging, in-vitro drug release and ex-vivo drug permeation. It was found that optimal formulation had a suitable gelation temperature at 31C  0.2C. It was observed that the system was fluid during nasal application at 25C and viscous at nasal temperature at 32C. RM-SLNs-GEL has shown particle size, polydispersity index PDI,  encapsulation efficiency EE; 253 nm, 0.282, 37.8 respectively. Ex-vivo permeation study exposed significant enhancement of permeability of RM-SLNs-GEL across mucosa than RM loaded thermosensitive gel RM-GEL. Our results show that RM-SLNs-GEL formulation could be a potential drug delivery system for the treatment of Parkinsons disease.

 Rasagiline mesylate RM is a selective irreversible MAO-B inhibitor used in the treatment of Parkinsons disease. This study was designed to prepare and optimize RM loaded solid lipid nanoparticles RM-SLNs in a thermosensitive mucoadhesive gel RM-SLNs-GEL. RM-SLNs were prepared combining Gelucire 5013 10, Labrasol 0.3 Cremophor RH40 12 with a mixing rate and time of 500 rpm, 45 min. Mucoadhesive gels were prepared combining Poloxamer 407 and HPMC E5 15.5  0.25. Optimized formulation RM-SLNs-GEL was evaluated for sol-gel transition temperature, viscosity, mucoadhesive force, particle size and distribution, SEM imaging, in-vitro drug release and ex-vivo drug permeation. It was found that optimal formulation had a suitable gelation temperature at 31C  0.2C. It was observed that the system was fluid during nasal application at 25C and viscous at nasal temperature at 32C. RM-SLNs-GEL has shown particle size, polydispersity index PDI,  encapsulation efficiency EE; 253 nm, 0.282, 37.8 respectively. Ex-vivo permeation study exposed significant enhancement of permeability of RM-SLNs-GEL across mucosa than RM loaded thermosensitive gel RM-GEL. Our results show that RM-SLNs-GEL formulation could be a potential drug delivery system for the treatment of Parkinsons disease.

 Rasagiline mesylate RM is a selective irreversible MAO-B inhibitor used in the treatment of Parkinsons disease. This study was designed to prepare and optimize RM loaded solid lipid nanoparticles RM-SLNs in a thermosensitive mucoadhesive gel RM-SLNs-GEL. RM-SLNs were prepared combining Gelucire 5013 10, Labrasol 0.3 Cremophor RH40 12 with a mixing rate and time of 500 rpm, 45 min. Mucoadhesive gels were prepared combining Poloxamer 407 and HPMC E5 15.5  0.25. Optimized formulation RM-SLNs-GEL was evaluated for sol-gel transition temperature, viscosity, mucoadhesive force, particle size and distribution, SEM imaging, in-vitro drug release and ex-vivo drug permeation. It was found that optimal formulation had a suitable gelation temperature at 31C  0.2C. It was observed that the system was fluid during nasal application at 25C and viscous at nasal temperature at 32C. RM-SLNs-GEL has shown particle size, polydispersity index PDI,  encapsulation efficiency EE; 253 nm, 0.282, 37.8 respectively. Ex-vivo permeation study exposed significant enhancement of permeability of RM-SLNs-GEL across mucosa than RM loaded thermosensitive gel RM-GEL. Our results show that RM-SLNs-GEL formulation could be a potential drug delivery system for the treatment of Parkinsons disease.

 Rasagiline mesylate RM is a selective irreversible MAO-B inhibitor used in the treatment of Parkinsons disease. This study was designed to prepare and optimize RM loaded solid lipid nanoparticles RM-SLNs in a thermosensitive mucoadhesive gel RM-SLNs-GEL. RM-SLNs were prepared combining Gelucire 5013 10, Labrasol 0.3 Cremophor RH40 12 with a mixing rate and time of 500 rpm, 45 min. Mucoadhesive gels were prepared combining Poloxamer 407 and HPMC E5 15.5  0.25. Optimized formulation RM-SLNs-GEL was evaluated for sol-gel transition temperature, viscosity, mucoadhesive force, particle size and distribution, SEM imaging, in-vitro drug release and ex-vivo drug permeation. It was found that optimal formulation had a suitable gelation temperature at 31C  0.2C. It was observed that the system was fluid during nasal application at 25C and viscous at nasal temperature at 32C. RM-SLNs-GEL has shown particle size, polydispersity index PDI,  encapsulation efficiency EE; 253 nm, 0.282, 37.8 respectively. Ex-vivo permeation study exposed significant enhancement of permeability of RM-SLNs-GEL across mucosa than RM loaded thermosensitive gel RM-GEL. Our results show that RM-SLNs-GEL formulation could be a potential drug delivery system for the treatment of Parkinsons disease.

Article Details

Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization

Authors:

Mahmut Ozan Toksoy

Publisher:

Marmara University

Main Topics:

Pharmaceutical Delivery Technologies

Journal:

Journal of Research in Pharmacy Vol.25 Issue 5, pp.702-714

Document Type:

Article

Publication Date:

6/2025

Document Language:

English

Document ID (Org No.):

2001346236

pISSN:

2630-6344

Rasagiline mesylate

solid lipid nanoparticle

thermosensitive mucoadhesive gel

full factorial design

ex- vivo permeation

Issues

Article Details

Development of rasagiline mesylate loaded solid lipid nanoparticles in a thermosensitive mucoadhesive gel: Formulation design using DoE, in-vitro and ex-vivo characterization

Authors: Mahmut Ozan Toksoy

Publisher: Marmara University

Main Topics: Pharmaceutical Delivery Technologies

Journal: Journal of Research in Pharmacy Vol.25 Issue 5, pp.702-714

Document Type: Article

Publication Date: 6/2025

Document Language: English

Document ID (Org No.): 2001346236

pISSN: 2630-6344

Rasagiline mesylate

solid lipid nanoparticle

thermosensitive mucoadhesive gel

full factorial design

ex- vivo permeation

Issues

Authors:

Mahmut Ozan Toksoy

Publisher:

Marmara University

Main Topics:

Pharmaceutical Delivery Technologies

Journal:

Journal of Research in Pharmacy Vol.25 Issue 5, pp.702-714

Document Type:

Article

Publication Date:

6/2025

Document Language:

English

Document ID (Org No.):

2001346236

pISSN:

2630-6344