RESUMEN
Aim: This study focused on developing a topical gel incorporating lornoxicam-loaded poly(lactic-co-glycolic acid) and polyethylene glycol (PLGA-PEG) blend nanoparticles to mitigate gastrointestinal (GIT) side effects and enhance therapeutic efficacy. Materials & methods: Synthesized nanoparticles were subjected to in vitro characterization, ex vivo permeation studies, and acute oral toxicity analysis post-incorporation into the gel using a S/O/W double emulsion solvent. Results & conclusion: The nanoparticles displayed a smooth, spherical morphology (170-321 nm) with increased entrapment efficiency (96.2%). LOX exhibited a permeation rate of 70-94% from the nanoparticle-infused gel, demonstrating favorable biocompatibility at the cellular level. The formulated gel, enriched with nanoparticles, holds promising prospects for drug-delivery systems and promising improved therapeutic outcomes for LOX.
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RESUMEN
Oral administration of BCS class IV anticancer agents has always remained challenging and frequently results in poor oral bioavailability. The goal of the current study was to develop hybrid nanoparticles (HNPs) employing cholesterol and poloxamer-407 to boost paclitaxel's (PTX) oral bioavailability. A series of HNPs with different cholesterol and poloxamer-407 ratios were developed utilizing a single-step nanoprecipitation technique. The PTX loaded HNPs were characterized systematically via particle size, zeta potential, polydispersity index, surface morphology, in vitro drug release, FTIR, DSC, XRD, acute oral toxicity analysis, hemolysis evaluation, accelerated stability studies, and in vivo pharmacokinetic analysis. The HNPs were found within the range of 106.6±55.60 - 244.5±88.24â¯nm diameter with the polydispersity index ranging from 0.20±0.03 - 0.51±0.11. SEM confirmed circular, nonporous, and smooth surfaces of HNPs. PTX loaded HNPs exhibited controlled release profile. The compatibility between the components of formulation, thermal stability, and amorphous nature of HNPs were confirmed by FTIR, DSC, and XRD, respectively. Acute oral toxicity analysis revealed that developed system have no deleterious effects on the animals' cellular structures. HNPs demonstrated notable cytotoxic effects and were hemocompatible at relatively higher concentrations. In vivo pharmacokinetic profile (AUC0-∞, AUMC0-∞, t1/2, and MRT0-∞) of the PTX loaded HNPs was improved as compared to pure PTX. It is concluded from our findings that the developed HNPs are hemocompatible, biocompatible and have significantly enhanced the oral bioavailability of PTX.
RESUMEN
This research aimed to enhance dermal delivery and optimize depigmentation therapy by designing mesoporous silica nanoparticles (MSNs) encapsulating azelaic acid (AZA) within a gel matrix. The MSNs were prepared using the sol-gel method. After subsequent processes, including acid extraction and drug loading, were then elucidated through PDI, size, zeta-potential, entrapment efficiency, nitrogen adsorption assay, FE-SEM, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and tyrosinase inhibition assay, were employed to assess the formulation. In-vitro stability tests for both AZA-MSN gel (AZCG) and AZA-loaded mesoporous silica gel (AZMG) were conducted at 8 °C, 25 °C, 40 °C, and 40 °C + 75 % RH, encompassing assessments of color, liquefaction, pH, and conductivity. Our findings showed a notable entrapment efficiency of 93.46 % for AZA-MSNs, with FE-SEM illustrating porous spherical MSNs. The particle size of AZA-MSNs was determined to be 211.9 nm, with a pore size of 2.47 nm and XRD analysis confirmed the amorphous state of AZA within the MSN carriers. Rheology examination indicated a non-Newtonian flow, while ex-vivo rat skin permeation studies conducted in a phosphate buffer (pH = 5.5) demonstrated a biphasic release pattern with 85.53 % cumulative drug permeation for AZA-MSNs. Overall, the study endorse the potential of AZA-MSNs as an efficacious and stable formulation for AZA delivery, highlighting their promise in addressing pigmentation concerns compared to conventional approaches.