Ocular disposition of ciprofloxacin from topical, PEGylated nanostructured lipid carriers: Effect of molecular weight and density of poly (ethylene) glycol

Abstract

Ciprofloxacin (CIP) is an antibacterial agent prescribed for the treatment of ocular infections. The objective of the present project is to investigate the effect of surface PEG functionalization of the Nano structured lipid carriers (NLCs) on formulation stability, ocular penetration and distribution. CIP NLCs were tested with different molecular weight (poly ethylene glycol) PEGs ranging from (2K to 20K) grafted onto the phospholipid and with different chain lengths (14–18 carbons) of phospholipids derivatized with PEG-2K. Drug load in the formulations was maintained at 0.3% w/v. Formulations prepared were evaluated with respect to in vitro release, transcorneal permeation, autoclavability, morphological characteristics and in vivo ocular tissue distribution. Scanning Transmission electron microscopy (STEM) studies revealed that the PEG-CIP-NLCs were spherical in shape. Transcorneal penetration of CIP was optimum with PEG molecular weight in between 2K to 10K. Carbon chain length of the phospholipid, however, did not affect transcorneal penetration of CIP. In vivo ocular tissue CIP concentrations attained from the various formulations was consistent with the in vitro data obtained. The results suggest that surface functionalization of PEGs, within a specified range of molecular weight and surface packing density, significantly enhance trans-ocular penetration and impart sterilization-stabilization characteristics into the formulations.

Development, Characterization and Antidiabetic Potentials of Nilgirianthusciliatus Nees Derived Nanoparticles

“…Biodegradable nanoparticles have been used frequently used as drug delivery vehicles due to their high bioavailability, good encapsulation properties, and relatively lack of toxicity [36]. Different nano-sized carriers, such as nanoparticles, polymeric micelles, liposomes, surface-modified nanoparticles and solid lipid nanoparticles [37][38][39][40], have been developed and suggested for achieving these goals. As the basis for a natural encapsulation agent, gelatin is widely used in a number of formulations because of its biocompatibility, biodegradability, and low antigenicity.…”

Application of nanostructured lipid carriers: the prolonged protective effects for sesamol in in vitro and in vivo models of ischemic stroke via activation of PI3K signalling pathway

“…In this respect, S-NLCs by potentiating the antioxidant defense system and attenuation of I/R-induced oxidative stress in the hippocampal region (Table 5 ) may exert promising neuroprotective effects. Indeed, NLC-based formulations are promising therapeutic candidates against a variety of pathological conditions including the ophthalmic disorders [ 71 , 72 ].…”

Topical Drug Delivery for Effective Treatment of Bacterial Infections of the Anterior Segment of the Eye

“…Numerous ocular delivery systems were developed to increase the bioavailability of ocular antibacterial drugs by prolonging their contact time with ocular surface [27,39] such as minitablets [40], ointments [41][42][43], ocuserts [44], microparticles [45], nanocarriers [46,47], collagen shields [48], in situ gel [49,50], microemulsions [51,52], contact lenses [53], and films [54][55][56]. Each system has its own advantages and limitations.…”