Comparison of Nanoemulsion and Aqueous Micelle Systems of Paliperidone for Intranasal Delivery

Abstract

The objective of the study was to develop and compare the efficiency of nanoemulsion and aqueous micelle system of Paliperidone on intranasal administration. Both the formulations were evaluated for physical parameters such as globule size, pH, viscosity, conductivity and in vitro drug release studies. The reduction in spontaneous motor activity of L-dopa and Carbidopa-treated Swiss Albino mice on intranasal administration of nanoemulsion and micellar system of Paliperidone was compared with plain drug suspension. Histopathological evaluation of formulation treated nasal mucosal membrane was performed. Nasal spray device was evaluated for spray pattern and volume per actuation. Globule size of micellar system and nanoemulsion was found to be 16.14 & 38.25 nm, respectively. In vitro release of drug from micellar system was found to be 1.8-fold higher than nanoemulsion. The loading of drug in nanoemulsion was found to be superior (2.5 mg/mL) when compared to micellar system (0.41 mg/mL). The spray pattern of micellar system and nanoemulsion from the device was elliptical and circular, respectively. The locomotor activity of L-dopa and Carbidopa-treated Swiss albino mice was found to be 1096.5±78.49, 551.5±13.43 and 535.5±24.75 counts/min in case of plain drug suspension, micellar system and nanoemulsion, respectively. The intranasal administration of developed formulations showed significant difference (p<0.01) in the locomotor activity when compared to intranasal administration of plain drug. Thus it can be concluded that both the developed formulations have shown improved in vivo activity on intranasal administration and pose great potential for delivery of Paliperidone through intranasal route.

Design and characterisation of colloidal nanocarriers for enhanced skin delivery of etodolac

“…The electrical conductivity measurements are facilitated for assessment of microemulsion type [14,23]. Mehta and Kaur [25] reported that very low specific conductivity (0.001-0.1 μS/cm) has presumed as water in oil (w/o) microemulsion, considering to conductivity of pure water (1.1-1.3 μS/cm) [26]. Based on this background, electrical conductivity data confirmed the generation of o/w types of microemulsions in the study (Table 1).…”

Antipsychotics-Loaded Nanometric Emulsions for Brain Delivery

“…Pidaparthi et al [ 29 ] also formulated paliperidone into an O/W nanometric emulsion for intranasal delivery. The nanoemulsion’s composition included Labrafil ® M 1944 CS (oleoyl polyoxyl-6 glyceride), Tween ® 80 (polysorbate 80-polyoxyethylene 20 sorbitan monooleate), Transcutol ® HP (diethylene glycol monoethyl ether), benzalkonium chloride and phosphate buffer (pH 6.4) (specific amounts in Table 6 ).…”

“…Paliperidone O/W intranasal nanometric emulsions were carried out in 2 studies. Despite having similar viscosities, the microemulsions developed by Patel et al [ 28 ] reached a higher drug strength, lower droplet size, good PDI, and were prepared by spontaneous emulsification, whereas the nanoemulsion developed by Pidaparthi et al [ 29 ] required more complex preparation methods and did not even report PDI values. Nevertheless, all formulations reportedly had therapeutic-like effects in pharmacodynamic studies (same animal model), despite the administered dose being 10 times less in the Pidaparthi et al case.…”

Fast In Vitro Release and In Vivo Absorption of an Anti-Schizophrenic Drug Paliperidone from Its Soluplus®/TPGS Mixed Micelles

“…Moreover, nanocrystals of aripiprazole incorporated into buccoadhesive chitosan films could also provide a rapid drug delivery to the systemic circulation [ 7 ]. Intranasal administration of PPD nanoemulsion and Tween 80—based micelles was reported to reduce the locomotor activity of mice more rapidly than that after administration of PPD suspension [ 8 ].…”