Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization

Abstract

Green nanotechnology utilizes the principles of green chemistry to formulate eco-friendly nanocarrier systems to mitigate patients and environment hazards. Raloxifene (RLX) demonstrates poor aqueous solubility (BCS class II) and low bioavailability, only 2% (extensive first-pass metabolism). The aim of this study is to enhance RLX solubility and bioavailability via development of novel solid dispersed multilayered core-sheath RLX-loaded nanofibers (RLX-NFs) without the involvement of organic solvents. A modified emulsion electrospinning technique was developed. Electrospinning of an RLX-nanoemulsion (RLX-NE) with polymer solution (poly vinyl alcohol (PVA), hydroxypropyl methylcellulose (HPMC), and chitosan (CS) in different volume ratios (1:9, 2:8, and 4:6) using D-optimal response surface methodology was adopted. In vitro characterization of RLX-loaded NFs was performed; scanning electron microscope (SEM), thermal analysis, drug content, release studies, and bioadhesion potential. The optimum NFs formula was evaluated for morphology using high-resolution transmission electron microscopy (HRTEM), and ex vivo drug permeation. The superiority of E2 (comprising RLX-NE and PVA (2:8)) over other NF formulae was statistically observed with respect to Q60 (56.048%), Q240 (94.612%), fiber size (594.678 nm), mucoadhesion time 24 h, flux (5.51 µg/cm2/h), and enhancement ratio (2.12). RLX pharmacokinetics parameters were evaluated in rabbits following buccal application of NF formula E2, relative to RLX oral dispersion. E2 showed significantly higher Cmax (53.18 ± 4.56 ng/mL), and relative bioavailability (≈2.29-fold).

Mercaptopurine-Loaded Sandwiched Tri-Layered Composed of Electrospun Polycaprolactone/Poly(Methyl Methacrylate) Nanofibrous Scaffolds as Anticancer Carrier with Antimicrobial and Antibiotic Features: Sandwich Configuration Nanofibers, Release Study and in vitro Bioevaluation Tests

“…These results established that the absence of drug loss during the electrospinning process and uniform distribution of the drug through 6-MP -loaded nanofiber scaffolds. This result is coupled with that achieved by El-Helaly et al, 48 who successfully loaded raloxifene onto different polymer nanofiber mats with efficiencies ranging from 92–103% dependent on the different composite ratio of NFs mats.…”

Core-Sheath Pt-CeO2/Mesoporous SiO2 Electrospun Nanofibers as Catalysts for the Reverse Water Gas Shift Reaction

“…Then, the solution is drawn to make a jet that finally results in NFs being deposited on a collector after drying the solvent out. Electrospun NFs have been utilized in a broad range of applications, such as gas sensing [ 8 ], filtration membranes [ 9 , 10 ], biomedicine [ 11 , 12 , 13 ], and catalysis [ 14 , 15 , 16 ]. ES as an engineering technique has the potential to produce NFs on a large scale that is a relative advantage of this technique compared to the batch chemical synthesis methods, which produce limited amounts of the material [ 17 , 18 ].…”

Microporation-Mediated Transdermal Delivery of In Situ Gel Incorporating Etodolac-Loaded PLGA Nanoparticles for Management of Rheumatoid Arthritis

“…The permeation of ETD was tested using USP dissolution tester apparatus (Hanson RS-8 plus, US) [41][42][43][44]. Skin was fitted in a cylindrical glass tube with an effective diffusional area of 0.785 cm 2 .…”