The contemporary research implicates the formulation and evaluation of a thermosensitive in situ nano gelling method to improve solubility and ocular residence time of flurbiprofen. This study was carried out in two phases. In the first phase, an insolubility drug has been formulated in the form of a nanoparticulate system and evaluated for its characteristics. The nanoparticles obtained demonstrated an average size array of 150 to 250 nm in diameter, up to 79.35% encapsulation efficiency, and up to 93.42% drug release throughout 2 h. In the second phase, nanoparticulate systems were dispersed in aqueous solutions of Pluronic F 127 (14%) and various concentrations of Carbopol 934 in combination to form an in situ nano gel. The prepared in situ gel was investigated for its physicochemical properties like pH, flowability, sol-gel transition temperature, gelling capacity, and rheological properties. Carbopol 934 did not significantly affect sol-gel transition temperature in optimized concentration (< 0.3%) but altered gelling capacity, pH, and transparency of the formulations. In vivo resident time and eye irritation test was evaluated in the rabbit eye. In optimized in situ gelling formulation (NIGF3), approximately 95% of in vitro drug release was observed after 6 h. NIGF3 increased precorneal residence time and high concentration in aqueous humor when paralleled to flurbiprofen eye drops. Greater concentration of drug in aqueous humor was due to its improved saturation solubility of the drug, and amplified residence time was attributed to the formation of gel matrix-embedded nanoparticles. This demonstrated that in situ nano gels (NIGF3) comprehending aqueous solutions of 0.3% w/v concentrations of Carbopol 934 with Pluronic F 127 may ominously persist the residence time and mend bioavailability of a water-insoluble drug. Graphical abstract
The purpose of the present research work was to design, optimize, and evaluate fluvastatin-loaded solid lipid nanoparticles (FLV-SLNPs) using 32 factorial design for enhancing the bioavailability. Fluvastatin has several disadvantages, including the low solubility and substantial first-pass metabolism resulting in a low (30%) bioavailability and a short elimination half-life. FLV-SLNPs were prepared using the nano-emulsion technique. For the optimization of the FLV-SLNPs, a total of nine formulations were prepared by varying two independent factors at three levels, using full factorial design. In this design, lipid (A) and surfactant (B) concentrations were chosen as independent factors, whereas entrapment efficiency (Y1) and in-vitro drug release (Y2) were selected as the dependent variables. Additionally, the prepared SLNPs were characterized for X-ray diffraction, Fourier transform-infrared spectroscopy, and differential scanning calorimetry. These studies revealed that there were no interactions between the drug and the selected excipients and the selected formulation components are compatible with the drug. Pharmacokinetic studies in rats confirmed significant improvement in AUC and MRT of SLNPs in comparison with the pure drug indicating the enhanced bioavailability of SLNPs. This study provides a proof-of-concept for the fact that SLNPs can be effectively developed via experimental factorial design, which requires relatively minimal experimentation.
Three Dimensional (3D) printing is a promising method for quick prototyping and manufacturing of any material. It is similar to photocopy or printing, where the new materials are formed on layers (3D) like their mother component. Following its growth and advancement in the 1980s, its application in pharmaceuticals is still limited. It has become one of the most innovative and influential tools serving as a technology for developing dosage forms from the last decade. The potential of 3D printing to produce drugs for precise measurement customized to specific patients' needs has shown the possibility of developing personalized medicines to novel dosage forms. The breakthrough allows the clear perception of the dosage structures on different shapes, sizes, surfaces and the associated challenges in delivering them by using such designed conditions. There are different difficulties related to the correct utilization of 3D imprinting in the pharmaceuticals, which have a strong impact on the scope of this technology. Recent advancements in the field of 3D printing technology used in the pharmaceutical industry mainly focused on different techniques for the fabrication of different dosage forms. The Food and Drug Administration's (FDA) recent approval of the first 3D prescription highlights possibilities for 3D printing innovation in the field of pharmaceutical drug supply. This analysis assesses 3D printing advancement possibilities, particularly in the area of custom prescriptions. This technology can be regarded as the future produced on demand, low-cost solid dosage forms and helps minimize side effects due to overdose.
1 June 2020 in Journal of Drug Delivery Science and Technology