Compritol®-based solid lipid nanoparticles of desvenlafaxine prepared by ultrasonication-assisted hot-melt encapsulation to modify its release.

Aims: Desvenlafaxine (DES) in conventional dosage forms shows initial burst release after oral administration, leading to exaggeration of its side effects. These side effects can be overcome by a sustained-release dosage form using the chemically inert, low-melting-point lipid Compritol® 888 ATO, as it reduces initial burst release. Materials & methods: The potential of DES-loaded solid lipid nanoparticles (DES-SLNs) synthesized by ultrasonication-assisted hot-melt encapsulation to modify the release of DES was investigated. Results: The entrapment efficiency of DES-SLNs was 65.90% with the in vitro release profile showing a sustained-release behavior achieving 81% cumulative release within 16 h without initial burst release. Conclusion: DES-SLNs are a potential carrier for sustained release of water-soluble antidepressant drugs such as DES.

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Phytochemical analysis and bioactivity assessment of five medicinal plants from Pakistan: Exploring polyphenol contents, antioxidant potential, and antibacterial activities.

Plants have always been the prime focus in medicine industries due to their enormous ethnobotanical uses and multitude of biological and therapeutic properties. In the current study, preliminary phytochemical composition, Total phenolic content (TPC), and total flavonoid content (TFC) with the antioxidant and antibacterial activity of hydroalcoholic extract and n-hexane, chloroform and n-butanol fractions of five selected medicinal plants [Tephrosia purpurea (L.) Pers., Lavandula stoechas L., Aesculus indica (Wall. ex Cambess.) Hook, Iris ensata Thunb., and Kalanchoe pinnata (Lam.) Pers.] from Pakistan, have been evaluated. TPC and TFC were determined by Folin-Ciocalteu's and AlCl3 methods respectively. The antioxidant activity was performed by DPPH, ABTS, FRAP, and CUPRAC while the antibacterial potential of these plants was determined by agar well diffusion assay. K. pinnata (Lam.) Pers. exhibited the highest TPC (695 ± 13.2 mg.GA.Eq.g-1DE ± SD) in n-butanol fraction and the highest TFC in its chloroform faction (615 ± 6.31 mg Q.Eq.g-1 DE ± SD). The n-butanol fraction and hydroalcoholic extract of I. ensata Thunb. exhibited strong antioxidant potential by DPPH and CUPRAC assays respectively, whereas K. pinnata (Lam.) Pers. n-butanol fraction exhibited the strongest reducing potential. The hydroalcoholic extract of all tested plants exhibited significant antibacterial activity against tested bacterial strains with ZI (12-18 mm). Conclusively, K. pinnata (Lam.) Pers. (Family: Crassulaceae) and I. ensataThunb. (Family: Iridaceae) exhibited the highest antioxidant and antibacterial potential. They can be explored for the isolation of phytoconstituents responsible for this potential and serve as a lead for the production of new natural antioxidants and antibacterial agents that can be used to cure various diseases.

Compritol-Based Alprazolam Solid Lipid Nanoparticles for Sustained Release of Alprazolam: Preparation by Hot Melt Encapsulation.

The current study was designed to investigate the feasibility of incorporating the water-insoluble lipophilic drug Alprazolam (Alp) into solid lipid nanoparticles (SLNs) to offer the combined benefits of the quick onset of action along with the sustained release of the drug. Therefore, compritol-based alprazolam-loaded SLNs (Alp-SLNs) would provide early relief from anxiety and sleep disturbances and long-lasting control of symptoms in patients with depression, thereby enhancing patient compliance. The optimized Alp-SLNs analyzed by DLS and SEM showed consistent particle size of 92.9 nm with PI values and standard deviation of the measurements calculated at <0.3 and negative surface charge. These characteristic values demonstrate the desired level of homogeneity and good physical stability of Alp-SLNs. The SLNs had a good entrapment efficiency (89.4%) and high drug-loading capacity (77.9%). SEM analysis revealed the smooth spherical morphology of the SLNs. The physical condition of alprazolam and absence of interaction among formulation components in Alp-SLNs was confirmed by FTIR and DSC analyses. XRD analysis demonstrated the molecular dispersion of crystalline alprazolam in Alp-SLNs. The in vitro release study implied that the release of Alp from the optimized Alp-SLN formulation was sustained as compared to the Alp drug solution because Alp-SLNs exhibited sustained release of alprazolam over 24 h. Alp-SLNs are a promising candidate to achieve sustained release of the short-acting drug Alp, thereby reducing its dosing frequency and enhancing patient compliance.