Medium and large scale preparation of Nanostructured Lipid Carriers of asenapine maleate: Quality-by-design based optimization, production, characterization and performance evaluation

Rao, Rajat Radhakrishna; Pisay, Muralidhar; Kumar, Sunil; Kulkarni, Sanjay; Pandey, Abhijeet; Kulkarni, Vijay; Mutalik, Srinivas

doi:10.1016/j.jddst.2022.103275

Cited by 3 publications

(1 citation statement)

References 41 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Over the years, several methods have been explored to enhance ASPM's pharmaceutical properties, bioavailability, and therapeutic e cacy. Gambhire et al (2018) developed Solid Lipid Nanoparticles to improve ASPM's bioavailability by bypassing rst-pass metabolism [5]. Researchers have conducted numerous studies to devise diverse formulations of Asenapine Maleate, such as sublingual lm [6], Thermo-reversible Mucoadhesive in situ Nasal Gel of Asenapine Maleate [7], nanostructured lipid carriers (NLCs) for intranasal Asenapine Maleate delivery to brain [8], and surface modi ed solid lipid nanoparticles loaded with Asenapine Maleate (SLN) [9,10].…”

Section: Introductionmentioning

confidence: 99%

Tailoring Nanostructured Lipid Carriers for Efficient Delivery of Asenapine Maleate in Antipsychotic Treatment

Rao,

Jamadar

2024

Preprint

View full text Add to dashboard Cite

Asenapine Maleate (ASPM), is the atypical antipsychotic agent used for treating various psychological disorders such as schizophrenia and acute mania associated with bipolar disorder. However, the drug's therapeutic potential is intricately linked to its solubility, bioavailability, stability, and ability to be delivered specifically to the central nervous system. The aim of the study was to design, develop, and optimize Nanostructured Lipid Carriers (NLCs) encapsulating Asenapine maleate to improve the therapeutic efficacy. The development utilized a systematic approach; various formulation parameters such as lipid composition, surfactant concentration, and entrapment efficiency were meticulously optimized by employing quality-by-design principles. The optimized ASPM-loaded NLCs demonstrated a particle size of 97.6 ± 2.48 nm, zeta potential of −20mV, and entrapment efficiency of 96.74%, respectively. ASPM-loaded NLC showed initially rapid release (20%) accompanied by sustained release (75%) over 24 hr with 22-fold improvement in oral bioavailability with significantly reduced locomotor count induced by L-DOPA-carbidopa in comparison with the pure drug in Sprague-Dawley rats. Furthermore, in-vitro and in-vivo results underscored the enhanced permeability through the blood-brain barrier with superior pharmacokinetics for the NLC. Collectively, this research elucidates the potential of optimized NLCs as robust drug delivery system for asenapine maleate, offering a promising avenue for advancing therapeutic results in the management of psychosis.

show abstract

Section: Introductionmentioning

confidence: 99%

Tailoring Nanostructured Lipid Carriers for Efficient Delivery of Asenapine Maleate in Antipsychotic Treatment

Rao,

Jamadar

2024

Preprint

View full text Add to dashboard Cite

show abstract

Optimization and evaluation of microwave-assisted curcumin-loaded nanostructured lipid carriers: a green approach

Lohan,

Verma,

Kaushik

et al. 2023

Futur J Pharm Sci

View full text Add to dashboard Cite

Background The goal of current research work is to develop and optimize curcumin-encapsulated nanostructured lipid carriers and to enhance therapeutic effect of curcumin after oral administration. Method Curcumin-loaded nanostructured lipid carriers were developed by a single-step one-pot microwave-assisted technique. The preparation of curcumin-loaded nanostructured lipid carriers was optimized by employing two factors and three levels central composite design (Design Expert® software) taking concentration of lipid blend and surfactant as independent variables and particle size, polydispersity index, and zeta potential as dependent variables, to investigate the effect of formulation ingredients on the physicochemical characteristics of nanostructured lipid carriers. The optimized batch was investigated by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, high-resolution transmission electron microscopy, in vitro drug release, stability studies, cytotoxicity, and in vivo anthelmintic studies. Results The average particle size, polydispersity index, and zeta potential of the optimized batch were found to be 144 nm, 0.301, and − 33.2 mV, respectively, with an entrapment efficiency of 92.48%. The results of high-resolution transmission electron microscopy confirmed spherical shape of particles. In vivo antiparasitic studies included determining the duration of paralysis and eventual death of earthworms in the presence of test samples. The results of in vivo studies showed good anthelmintic potential for curcumin-loaded nanostructured lipid carriers as compared to albendazole in different concentrations. Cytotoxicity studies also confirmed the formulation to be nontoxic to Vero cells. In vitro drug release study showed 90.76 ± 0.01% release of curcumin in 24 h by following the Korsmeyer-Peppas model of release kinetics. Conclusion The aforementioned results imply that microwave-developed nanostructured lipid carriers could be promising drug carriers and will aid in their fabrication for oral administration as a possible alternative for the treatment of other parasitic infections. Graphical Abstract

show abstract

Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach

et al. 2022

View full text Add to dashboard Cite

Medium and large scale preparation of Nanostructured Lipid Carriers of asenapine maleate: Quality-by-design based optimization, production, characterization and performance evaluation

Cited by 3 publications

References 41 publications

Tailoring Nanostructured Lipid Carriers for Efficient Delivery of Asenapine Maleate in Antipsychotic Treatment

Tailoring Nanostructured Lipid Carriers for Efficient Delivery of Asenapine Maleate in Antipsychotic Treatment

Optimization and evaluation of microwave-assisted curcumin-loaded nanostructured lipid carriers: a green approach

Development of Novel Solid Nanostructured Lipid Carriers for Bioavailability Enhancement Using a Quality by Design Approach

Contact Info

Product

Resources

About