<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Abstract

This study aimed to prepare solid self-nanoemulsified drug delivery system (S-SNEDDS) of lamotrigine (LMG) for enhancing its dissolution and oral bioavailability (BA). Methods: Nineteen liquid SNEDDS were prepared (R1-R19) using D-optimal design with different ratios of oil, surfactant (S), and cosurfactant (Cos). The formulations were characterized regarding robustness to dilution, droplet size, thermodynamic stability testing, selfemulsification time, in-vitro release in 0.1 N HCl and phosphate buffer (PB; pH 6.8). Design Expert ® 11 software was used to select the optimum formulations. Eight S-SNEDDS were prepared (S1-S8) using 2 3 factorial design, and characterized by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and scanning electron microscopy (SEM). The optimum formulation was chosen regarding in-vitro drug released in 0.1 N HCl and PB, compared to pure LMG and commercial tablet (Lamictal ®). The BA of LMG from the optimized S-SNEDDS formulation was evaluated in rabbits compared to pure LMG and Lamictal ®. Results: The optimized S-SNEDDS was S2, consisting of R9 adsorbed on Aeroperl ® 300 in a ratio of 1:1, with the best results regarding in-vitro drug released in 0.1 N HCl at 15 min (100%) compared to pure LMG (73.40%) and Lamictal ® (79.43%), and in-vitro drug released in PB at 45 min (100%) compared to pure LMG (30.46%) and Lamictal ® (92.08%). DSC, PXRD, and SEM indicated that LMG was molecularly dispersed within the solid nano-system. The BA of S2 was increased 2.03 and 1.605 folds compared to pure LMG, and Lamictal ® , respectively. Conclusion: S2 is a promising S-SNEDDS formulation. It can be a potential carrier for improving dissolution, and BA of LMG.

3D Printing of Dapagliflozin Containing Self-Nanoemulsifying Tablets: Formulation Design and In Vitro Characterization

“…The drug release kinetics from 3D printed self-nanoemulsifying tablet formulation was best described by the Higuchi model. This observation aligns with the previously published literature report related to drug release kinetic behavior for a solid-SNEDDS [47]. The developed formulation system exhibited the best linearity and regression coefficient values of 0.986 with a release exponent (n) value of 0.191 for the tablet of 8 mm size whereas the regression coefficient and n value for the tablet of 10 mm and 12 mm diameters were 0.980 with n value of 0.265 and 0.985 with n value of 0.221, respectively.…”

Self-Emulsifying Drug Delivery Systems: An Alternative Approach to Improve Brain Bioavailability of Poorly Water-Soluble Drugs through Intranasal Administration

“…An example of this dependence is given by the Abdelmonem et al [ 23 ] study, describing a faster release of lamotrigine from SNEDDS in a 0.1 N HCl medium than when placed in a PBS medium. This difference between release profiles is explained by the pH-dependent solubility of lamotrigine [ 23 ]. Another example of this dependence is the case of ferulic acid release from a SMEDDS, which was approximately 80% in a pH 1.2 medium but 100% in a phosphate buffer pH 6.8 medium [ 31 ].…”

“…Once more, a point worth being discussed is that in the literature, the authors’ classification of SEDDS excipients as surfactants or cosurfactants does not always correspond to the expected. A clear example is the Tween 80 classification as a cosurfactant made by different authors [ 23 , 24 , 25 ] that, in reality, is a hydrophilic surfactant with an HLB of 15. So, for a better harmonization of excipients classification, in Figure 1 and Table 1 we considered as surfactants the hydrophilic surfactants with an HLB > 10, and as cosurfactants the organic solvents and hydrophobic surfactants (HLB < 10) used in addition to oils (sometimes hydrophobic surfactants are used as the oil component).…”

“…A small number of SEDDS-based products have already been successfully introduced into the pharmaceutical market, with none of them loading drugs for the treatment of neurological disorders. Until now, several in vivo assays using oral SEDDS have been carried out for neuropharmaceuticals brain targeting [ 4 , 6 , 23 , 24 , 25 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 70 ], but only a few in vivo pre-clinical studies have been reported for IN administration of neurotherapeutics loaded in SEDDS. In fact, only six studies were found that investigated the IN administration of neurotherapeutics loaded in SEDDS: clonazepam [ 45 ], diazepam [ 44 ], and perampanel [ 28 ] for epilepsy treatment; Bdph for glioblastoma treatment [ 4 ]; huperzine A [ 30 ] for Alzheimer’s disease; and naringin [ 5 ] as a neuroprotective for Alzheimer’s and Parkinson’s disease.…”

Preparation and <i>in vitro</i> tumor growth inhibitory effect of oligo (L-lactate) nanoparticles

“…Thus, it can be a strategy for formulating nanoparticles by increasing the cellular uptake of water-insoluble macromolecules. Several techniques for reducing particle size have been proposed, including micro/nanomization (7-10), solubilization (11,12), and self-emulsification (13)(14)(15)(16). Among the size reduction methods, the solvent diffusion method is often used for preparing polymeric nanoparticles (17)(18)(19)(20)(21).…”