<p>Preparation of sustained release apremilast-loaded PLGA nanoparticles: in vitro characterization and in vivo pharmacokinetic study in rats</p>

Abstract

Background Apremilast (APM) is a novel, orally administered small molecule drug approved for treatment of psoriasis or psoriatic arthritis. Due to its low solubility and permeability, it is classified as a class IV drug according to BCS classification. Dose titration is recommended during APM treatment due to its tolerability and twice-daily dosing regimen issues. Materials and Methods In this study, three different APM-loaded PLGA nanoparticles (F1–F3) were prepared by single emulsion and evaporation method. Based on particle size, PDI, zeta potential (ZP), entrapment efficiency (%EE), drug loading (%DL), and spectral characterization, the nanoparticles (F3) were optimized. The F3 nanoparticles were further evaluated for in vitro release and in vivo pharmacokinetic studies in rats. Results The optimized nanoparticles (F3) had particles size 307.3±8.5 nm with a low PDI value 0.317, ZP of −43.4±2.6 mV, EE of 61.1±1.9% and DL of 1.9±0.1%. The in vitro release profile showed a sustained release pattern of F3 nanoparticles of APM. The pharmacokinetic results showed 2.25 times increase in bio-availability of F3 nanoparticles compared to normal APM suspension. Moreover, significant increase in half-life and mean residence time confirms long-term retention of F3 nanoparticles. Conclusion Bioavailability enhancement along-with long-term retention of the APM-loaded PLGA nanoparticles might be helpful for the once-daily regimen treatment.

Ecofriendly densitometric RP-HPTLC method for determination of rivaroxaban in nanoparticle formulations using green solvents

“…Preparation and characterization of rivaroxaban loaded PLGA NPs Rivaroxaban loaded PLGA NPs formulation was prepared by solvent evaporation technique. 36 The formulation composition and characterization parameters of prepared NPs are summarized in Table 1. The purpose of preparation of PLGA NPs was to apply the proposed analytical methodology for the determination of rivaroxaban in NPs formulation.…”

“…Preparation of rivaroxaban loaded PLGA NPs "Emulsion solvent evaporation method" was used for the preparation rivaroxaban loaded PLGA NPs. 36 Briey, an accurately weighed amount of rivaroxaban (20 mg) was dissolved in 4 mL of PLGA polymeric solution in dichloromethane (DCM). Separately, aqueous phases were prepared by dissolving the required amount of polyvinyl alcohol (PVA) (500 mg) in distilled water (8 mL).…”

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

“…Prepared L-P-NPs were evaluated for particle size, polydispersity index (PDI) and zeta potential (ZP). The mean size and PDI of L-P-NPs (F1-F3) were measured using Malvern zeta sizer (ZEN-3600, Malvern Instruments Ltd., Holtsville, NY, USA) at 25 ± 2 • C, and dynamic light scattering (DLS) was set 90 • [28]. The freshly prepared DFL-loaded L-P-NPs dispersion was diluted (100 times) with double-distilled water and sonicated for 10 min.…”

Nanodermatology‐based solutions for psoriasis: State‐of‐the art and future prospects

“…Recently, Anwer et colleagues tested a Poly(D,L‐lactide‐coglycolide) (PLGA) nanocapsules loaded with apremilast (size = 307.3 ± 8.5 nm, PDI = 0.317, Z = −43.4 ± 2.6 mV) obtaining a 2.25 fold the serum concentration compared with the commercial apremilast pharmaceutical form (Anwer et al, ).…”