Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine

Abstract

This study reports on L-carnosine phytosomes as an alternative for the prodrug N-acetyl-L-carnosine as a novel delivery system to the lens. L-carnosine was loaded into lipid-based phytosomes and hyaluronic acid (HA)-dispersed phytosomes. L-carnosine-phospholipid complexes (PC) of different molar ratios, 1:1 and 1:2, were prepared by the solvent evaporation method. These complexes were characterized with thermal and spectral analyses. PC were dispersed in either phosphate buffered saline pH 7.4 or HA (0.1% w/v) in phosphate buffered saline to form phytosomes PC1:1, PC1:2, and PC1:2 HA, respectively. These phytosomal formulations were studied for size, zeta potential, morphology, contact angle, spreading coefficient, viscosity, ex vivo transcorneal permeation, and cytotoxicity using primary human corneal cells. L-carnosine-phospholipid formed a complex at a 1:2 molar ratio and phytosomes were in the size range of 380–450 nm, polydispersity index of 0.12–0.2. The viscosity of PC1:2 HA increased by 2.4 to 5-fold compared with HA solution and PC 1:2, respectively; significantly lower surface tension, contact angle, and greater spreading ability for phytosomes were also recorded. Ex vivo transcorneal permeation parameters showed significantly controlled corneal permeation of L-carnosine with the novel carrier systems without any significant impact on primary human corneal cell viability. Ex vivo porcine lenses incubated in high sugar media without and with L-carnosine showed concentration-dependent marked inhibition of lens brunescence indicative of the potential for delaying changes that underlie cataractogenesis that may be linked to diabetic processes.

Investigation of a new horizon antifungal activity with enhancing the antimicrobial efficacy of ciprofloxacin and its binary mixture via their encapsulation in nanoassemblies: in vitro and in vivo evaluation

“…NAC IR spectra showed a distinctive vibrational type of peaks (Figure c) in the region with elevated frequency including an expansion vibration at 3,237 and 3,049 cm −1 for the –CON–H (amide hydrogen) and NH3+ (protonated terminal amine) related to free l ‐carnosine, respectively. However, other remarkable peaks were recognized at 2,162 and 1,643 cm −1 that are caused by the N–H vibrational bending of amide group and imidazole stretching sequentially (Abdelkader et al, ). In the FT‐IR spectra of CIP nanosponges or its binary mixture with NAC, it was observed that the characteristic peaks of Cipro and/or NAC in the fingerprint region, that is, 3,524, 3,237, and 3,049 cm −1 were masked and cannot be distinguished from that of HPβ‐CD to appear as a single broad peak suggesting definite interactions between drugs and nanosponges (Swaminathan et al, ).…”

“…CIP showed sharp peaks at diffraction angles of 12, 20, and 27° suggesting its crystalline nature (Mallikarjuna et al, ; Sahoo, Chakraborti, & Mishra, ). Within this pursue, NAC was considered as a typical high crystallinity drug, due to its sharp X‐ray peaks, where at 20, 22.8, and 25° diffractive angles, the main distinctive peaks of NAC were revealed (Abdelkader et al, ). A comparative analysis of diffractograms of individual components and nanosponge formulations showed that the diffractograms of nanosponge formulations (C1, C2, C5, CA5, and CA6) are almost identical to that of HPβ‐CD, and it is hard to distinguish the characteristic crystallinity peaks of the pure drugs.…”

Novel Nanocarriers for Ethnopharmacological Formulations

“…The prepared phytosome using sinigrin shows higher efficiency than control to release the compound in a slow and controlled manner into the stratum corneum for wound healing [51]. Abdelkader et al formulated L-carnosine phytosome by combining hydrogel and lipid-based carrier which shows sustained drug pervasion and inhibits the browning of the lens and protects from cataract formation [52]. Damle et al focused on encapsulating orange peel and liquorice extracts into phospholipid complex which exhibited as a better topical dosage delivery towards skin that ensured high cutaneous absorption of phytoconstituents in the skin for long period of action in contradiction to skin ageing [53].…”

Untitled

“…Hyaluronic acid phytosomes loaded with L-carnosine was prepared by Abdelkader et al [44] in different molar ratios by solvent evaporation technique, where the prepared phytosomes showed ex vivo transcorneal permeation of L-carnosine loaded phytosome without affecting human corneal cell viability.…”