Proof-of-concept for Site-specific Delivery of Mesalamine Nanoparticles for Effective Therapy in Colitis

Sreeharsha, Nagaraja; Narayan, R. H.; Vijaya, Joshi; Nair, Anroop B.

doi:10.5530/ijper.55.2s.116

Cited by 2 publications

(1 citation statement)

References 11 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The particle size using a nano-size analyzer (Nanophox, Sympatec India Pvt. Ltd., Mumbai, India) at ambient temperature [ 18 ]. Zeta potential was measured on Delsa Nano C, Beckman Coulter zeta meter (LabIndia, Mumbai, India) [ 19 ].…”

Section: Methodsmentioning

confidence: 99%

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

2022

Self Cite

View full text Add to dashboard Cite

As regulatory and technical landscapes for pharmaceutical formulation development are rapidly evolving, a risk-management approach using multivariate analysis is highly essential for designing a product with requisite critical quality attributes (CQA). Efinaconazole, a newly approved poorly water-soluble antifungal triazole drug has poor permeability. Spanlastics, new-generation surfactant nanovesicles, being fluidic, help improve the permeability of drugs. Therefore, we optimized efinaconazole spanlastics using the concepts of Formulation-by-Design (FbD) and explored the feasibility of transungual delivery for the management of onychomycosis. Using the Ishikawa fishbone diagram, the risk factors that may have an impact on the CQA of efinaconazole spanlastic vesicles were identified. Application of the Plackett–Burman experimental design facilitated the screening of eight different formulation and process parameters influencing particle size, transmittance, relative deformability, zeta potential, entrapment efficiency, and dissolution efficiency. With the help of Pareto charts, the three most significant factors were identified, viz., vesicle builder (Span), edge activator (Tween), and mixing time. The levels of these three critical variables were optimized by FbD to reduce the particle size and maximize the transparency, relative deformability, encapsulation efficiency, and dissolution efficiency of efinaconazole spanlastic nanovesicles. Bayesian and Lenth’s analysis and mathematical modeling of the experimental data helped to quantify the critical formulation attributes required for getting the formulation with optimum quality features. The optimized efinaconazole-loaded spanlastic vesicles had a particle size of 197 nm, transparency of 91%, relative deformability of 12.5 min, and dissolution efficiency of 81.23%. The spanlastic formulation was incorporated into a gel and explored ex vivo for transungual delivery. This explorative study provides an example of the application of principles of risk management, statistical multivariate analysis, and the FbD approach in developing efinaconazole spanlastic nanovesicles.

show abstract

Section: Methodsmentioning

confidence: 99%

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

2022

Self Cite

View full text Add to dashboard Cite

show abstract

Mesalamine loaded ethyl cellulose nanoparticles: optimization and in vivo evaluation of antioxidant potential in ulcerative colitis

Gautam,

Akhter,

Anand

et al. 2024

Biomed. Mater.

View full text Add to dashboard Cite

This study aimed to optimize MES-nanoparticles using Box Behnken Design (BBD) and investigate its in vivo antioxidant potential in colon drug targeting. The formulation was prepared using oil/water (O/W) emulsion solvent evaporation technique for time dependent colonic delivery. The optimal formulation with the following parameters composition was selected: polymer concentration (% w/w) (A) = 0.63, surfactant concentration (% w/w) (B) = 0.71, sonication duration (min) (C) = 6. The outcomes showed that ethyl cellulose nanoparticle containing mesalamine has particles size of 142 ± 2.8 nm, zeta potential of -24.8 ± 2.3 mV, % EE of 87.9 ± 1.6%, and PDI of 0.226 ± 0.15. Scanning electron microscopy revealed nanoparticles has a uniform and spherical shape. The in-vitro release data disclosed that the ethyl cellulose nanoparticles containing mesalamine showed bursts release of 52±1.6% in simulated stomach media within 2 hours, followed by a steady release of 93±2.9% in simulated intestinal fluid that lasted for 48 hours. The mesalamine release from nanoparticle best match with the Korsmeyer-Peppas model (R2 = 0.962) and it followed fickian diffusion case I release mechanism. The formulation stability over six-months at 25 ± 2 °C with 65 ± 5% relative humidity, and 40 ± 2 °C with 75 ± 5% relative humidity showed no significant changes changes in colour, entrapment efficiency, particle sizes and zeta potential. As per in vivo results, MES-NP effectively increased GSH, SOD level and reduces the LPO level as compared to other treatment groups. The findings hold promise that the developed formulation can suitably give in ulcerative colitis.

show abstract

Proof-of-concept for Site-specific Delivery of Mesalamine Nanoparticles for Effective Therapy in Colitis

Cited by 2 publications

References 11 publications

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

Mesalamine loaded ethyl cellulose nanoparticles: optimization and in vivo evaluation of antioxidant potential in ulcerative colitis

Contact Info

Product

Resources

About