Ocular Delivery of Bimatoprost-Loaded Solid Lipid Nanoparticles for Effective Management of Glaucoma

Abstract

Glaucoma is a progressive optic neuropathy characterized by a rise in the intraocular pressure (IOP) leading to optic nerve damage. Bimatoprost is a prostaglandin analogue used to reduce the elevated IOP in patients with glaucoma. The currently available dosage forms for Bimatoprost suffer from relatively low ocular bioavailability. The objective of this study was to fabricate and optimize solid lipid nanoparticles (SLNs) containing Bimatoprost for ocular administration for the management of glaucoma. Bimatoprost-loaded SLNs were fabricated by solvent evaporation/ultrasonication technique. Glyceryl Monostearate (GMS) was adopted as solid lipid and poloxamer 407 as surfactant. Optimization of SLNs was conducted by central composite design. The optimized formulation was assessed for average particle size, entrapment efficiency (%), zeta potential, surface morphology, drug release study, sterility test, isotonicity test, Hen’s egg test-chorioallantoic membrane (HET-CAM) test and histopathology studies. The optimized Bimatoprost-loaded SLNs formulation had an average size of 183.3 ± 13.3 nm, zeta potential of −9.96 ± 1.2 mV, and encapsulation efficiency percentage of 71.8 ± 1.1%. Transmission electron microscopy (TEM) study revealed the nearly smooth surface of formulated particles with a nano-scale size range. In addition, SLNs significantly sustained Bimatoprost release for up to 12 h, compared to free drug (p < 005). Most importantly, HET-CAM test nullified the irritancy of the formulation was verified its tolerability upon ocular use, as manifested by a significant reduction in mean irritation score, compared to positive control (1% sodium dodecyl sulfate; p < 0.001). Histopathology study inferred the absence of any signs of cornea tissue damage upon treatment with Bimatoprost optimized formulation. Collectively, it was concluded that SLNs might represent a viable vehicle for enhancing the corneal permeation and ocular bioavailability of Bimatoprost for the management of glaucoma.

Preparation of hydrophobic layered double hydroxide-based composite pigments via octyltriethoxysilane surface modification for cosmetic applications

“…The two O/Dye-LDH pigments were predicted with eye irritation potential in the HET-CAM assay by recording the morphological changes in the CAM, including vascular lysis, coagulation and hemorrhage. 41 In addition, the calculated mean values of the cumulative scores are presented in Table 4. As shown in Fig.…”

Evaluation of Drug-Loaded and Surface-Adsorbed DNase/Tween-80 Solid Lipid Nanoparticles against Staphylococcus aureus Biofilms

“…For the TEM study, SLNs were diluted with HPLC-grade water, and one drop of SLNs was placed on a copper grid coated with a carbon film, followed by staining with phosphotungstic acid. The grid was vacuum-dried at ambient temperature and examined under TEM at an acceleration voltage of 100 kV. , …”

“…The grid was vacuum-dried at ambient temperature and examined under TEM at an acceleration voltage of 100 kV. 14,15 2.5. Fourier Transform Infrared (FTIR) Spectroscopy Analysis.…”

Drug Release from Lipid Microparticles—Insights into Drug Incorporation and the Influence of Physiological Factors

“…Research on lipid particles intended for ocular administration is practically limited to SLN. These studies were carried out using a modified Franz diffusion cell, a USP dissolution apparatus with modifications, or a modified rotating paddle dialysis bag diffusion technique, and simulated tear fluid (STF) as a release medium [ 22 , 23 , 24 , 25 ]. The composition of STF used in these studies was limited to 3–4 salts (usually NaCl, NaHCO 3 , CaCl 2 , KCl) and no enzymes were used.…”