Development and evaluation of cationic nanostructured lipid carriers for ophthalmic drug delivery of besifloxacin

Baig, MS; Owida, H; Njoroge, W; Siddiqui, AUR; Yang, Y

Abstract

Besifloxacin hydrochloride (BSF) is a new ophthalmic antibiotic. However, its low water solubility limits its therapeutic efficacy. This article reported a novel lipid based drug delivery system to enhance ocular bioavailability of BSF. Cationic nanostructured lipid carriers (CNLC) were prepared and optimized by Box-Behnken design via using Design Expert Software (R). Effect of concentration of three independent variables, Stabilizer, Solid lipid and Liquid Lipid were studied on three dependent variables Particle size, Polydispersity Index (PDI) and zeta potential of the CNLC particles. The surfactant, hexadecyltrimethylammonium bromide (CTAB) was used to optimize the surface charge of the nano-particles. The BSF loaded nano-particles, CNLC-BSF, were characterized fully. Rhodamine was trapped into CNLC-BSF for imaging. The cytotoxicity and cellular infiltration of CNLC-BSF were assessed by 2-dimensional (2D) and 3-dimensional (3D) conjunctival tissue model. It was revealed that the CNLC's parameters, particle size, PDI and zeta potential, remained stable over 2-week storage period. The entrapment efficiency was around 80% for optimum formulation. The cell internalization of CNLC increased when CTAB concentration increased in CNLC-BSF. The formulation showed good penetration property through the 3D tissue model. The cytotoxicity assessed by MIT assay showed minimum 60% cell viability on conjunctival fibroblast model for the optimized formula with inclusion of 0.6 mg/mL BSF.

Keywords: Cationic nanostructured lipid carrier; CNLC; Ophthalmic drug delivery; Bioavailability; Infiltration; Besifloxacin; Box-Behnken; Design-Expert

Related products/services

Liposomes for DNA/RNA Delivery

Liposomes are a type of biological nanocarrier commonly used for DNA/RNA delivery. Its structure consists of an aqueous core surrounded by a hydrophobic lipid layer, which effectively packages and protects DNA or RNA molecules. Liposomes bind to nucleic acids through charge interactions or fusion of lipid membranes, and form liposome-cell interactions on the cell membrane, promoting the internal release of nucleic acids. The liposome delivery system has good biocompatibility and low toxicity, and can effectively guide DNA/RNA into cells across biological barriers, such as cell membranes. This method has potential applications in gene therapy, vaccine development and other fields, and provides a feasible means for targeted therapy. However, liposome delivery systems still face some challenges, such as insufficient local concentration and immune activation. Continuous research efforts aim to optimize the design of liposomes to improve their delivery efficiency and biological stability, promoting their widespread application in the field of gene delivery.