Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

PubMed ID: 24451076Coenzyme Q10 (Q10) loaded solid lipid nanoparticles (SLN) were prepared by the high speed homogenization method and incorporated into Carbopol 974P hydrogels. Compritol 888 ATO (C888) was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw80) were used as surfactant and co-surfactant. Optimum particle size with narrow distribution was obtained as 152.2 nm for blank and 142.4 nm for Q10 loaded SLNs. The overall charge of loaded SLNs was-13.7 ± 1.3 mV. Q10 entrapment efficiency was 89 % and the production yield was 94 %. Transmission electron microscopy analysis provided evidence of colloidal size, spherical shape while differential scanning calorimetry analysis confirmed recrystallization of the lipid after the preparation of SLNs. Trolox equivalent antioxidant capacity (TEAC) analysis has shown that antioxidant potential of Q10 can be protected in SLNs. Rheological characteristics demonstrated that the SLN incorporating gels were shear thinning and the mechanical strength of the gels was suitable for topical application. Diffusion studies from rat abdominal skin revealed that the delivery of Q10 was doubled in SLN incorporating gels, approximately 40 µg cm-2, in comparison with gels prepared with only Q10 (not incorporated in SLNs). As a result, it can be stated that Q10- -SLN loaded gels can be successful delivery systems for carrying Q10 efficiently into the skin without losing its antioxidant properties.Scientific Research Foundation of Beijing Normal University: 09/ECZ/030Acknowledgement. – This study was supported by the University of Ege Scientific Research Foundation, Project No. 09/ECZ/030. -

Current status of chitosan on dermal/transdermal drug delivery systems

In case of targeting the drug to the desired part of the skin, vehicles play animportant role, beside the characteristics of the drug. Many natural and synthetic vehicleshave been used for various topical dermal/transdermal preparations. However, chitosanhas been standing out with its many advantages based mainly on its biological andphysicochemical properties. Chitosan is a unique hydrophilic biopolymer obtained bypartial deacetylation of chitin, which is one of the most abundant polysaccharide. It is anatural product widely found in crustacean shells, fungal cell walls, insect exosceletons,and mollusks. Chitosan is a linear glycosaminoglycan made up of N-acetyl-Dglucosamineunits.Characteristics of chitosan, such as the molecular weight, viscosity and the degree ofdeacetylation, greatly influence the properties of formulations. The by-products formedafter the biodegradation of the polymer does not cause immune responses making itbiocompatible. Due to the specific cationic glucosamine groups of chitosan, it can beinteracted with anionic proteins in the skin providing the bioadhesive characteristics.These properties result in improved efficacy, enhanced bioavailability and reducedtoxicity-generally recognized as safe (GRAS). Furthermore, the antimicrobial/antibacterial and skin hydrating effects of chitosan have been received considerableattention for dermal/transdermal applications. It plays an important role in the cell regulation, tissue regeneration and collagen production. Chitosan and some of itscomplexes were approved by FDA for use in wound dressing products.Chitosan also provides the controlled release of numerous active agents used for thetreatment of skin diseases such as corticosteroids, antifungal agents, nonsteroidal antiinflammatorydrugs, hormones, local anesthetics, antiviral and antiseptic agents, etc.Regarding to the good bioadhesive property of chitosan and its ability to sustain therelease of the active compounds, it has found many practices in the formulation of gels,dermal/transdermal patches, sponges, micro-and nanoparticulate systems as drugcarriers. Particularly, chitosan has been used in the preparation of mucoadhesiveformulations, for improving the dissolution rate of the poorly soluble drugs, drugtargeting and enhancement of peptide absorption.This paper is focused on the use of chitosan for dermal/ transdermal drug deliverysystems following a general overview of chitosan. This natural polymer is a promisingcarrier or excipient as a delivery system and remarkable advances have been made aboutits potential applications in skin delivery. © 2011 by Nova Science Publishers, Inc. All rights reserved

A Novel Alternative for the Treatment of Diabetic Foot Wounds: A Three Dimensional Porous Dermal Matrix

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A comparative evaluation of coenzyme Q10-loaded liposomes and solid lipid nanoparticles as dermal antioxidant carriers

PubMed ID: 23055723Background: The effective delivery of coenzyme Q10 (Q10) to the skin has several benefits in therapy for different skin pathologies. However, the delivery of Q10 to deeper layers of skin is challenging due to low aqueous solubility of Q10. Liposomes and solid lipid nanoparticles (SLN) have many advantages to accomplish the requirements in topical drug delivery. This study aims to evaluate the influence of these nanosystems on the effective delivery of Q10 into the skin. Methods: Q10-loaded liposomes (LIPO-Q10) and SLNs (SLN-Q10) were prepared by thin film hydration and high shear homogenization methods, respectively. Particle size (PS), polydispersity index (PI), zeta potential (ZP), and drug entrapment efficiency were determined. Differential scanning calorimetry analysis and morphological transmission electron microscopy (TEM) examination were conducted. Biocompatibility/cytotoxicity studies of Q10-loaded nanosystems were performed by means of cell culture (human fibroblasts) under oxidative conditions. The protective effect of formulations against production of reactive oxygen species were comparatively evaluated by cytofluorometry studies. Results: PS of uniform SLN-Q10 and LIPO-Q10 were determined as 152.4 ± 7.9 nm and 301.1 ± 8.2 nm, respectively. ZPs were -13.67 ± 1.32 mV and -36.6 ± 0.85 mV in the same order. The drug entrapment efficiency was 15% higher in SLN systems. TEM studies confirmed the colloidal size. SLN-Q10 and LIPO-Q10 showed biocompatibility towards fibroblasts up to 50 µM of Q10, which was determined as suitable for cell proliferation. The mean fluorescence intensity % depending on ROS production determined in cytofluorometric studies could be listed as Q10 ? SLN-Q10 > LIPO-Q10. Conclusion: The LIPO-Q10 system was able to enhance cell proliferation. On the contrary, SLN-Q10 did not show protective effects against ROS accumulation. As a conclusion, liposomes seem to have advantages over SLN in terms of effective delivery of Q10 to skin for antioxidant purposes. © 2012 Gokce et al, publisher and licensee Dove Medical Press Ltd

Cyclosporine A loaded SLNs: Evaluation of cellular uptake and corneal cytotoxicity

Cyclosporine A (CsA) loaded solid lipid nanoparticles (SLNs) for topical ophthalmic applications were prepared by high shear homogenization and ultrasound method using Compritol 888 ATO, Poloxamer 188 and Tween 80, to investigate the cellular uptake of rabbit corneal epithelial cells (RCE) and to evaluate the cytotoxicity. The size of the optimized formulation was 225.9±5.5nm with a polydispersity index of 0.253±0.05. The zeta potential and entrapment efficiency was detected as −16.9±0.7mV and 95.6%, respectively. The CsA release was found to be enzyme (lipase/co-lipase complex) dependent. SLNs were sterilized at 110 and 121 ◦C. The cytotoxicity was evaluated in vitro by means of RCE cells and was higher at 121 ◦C sterilization temperature, probably due to a supposed leakage of Tween 80 following lipid recrystallization. The permeation and penetration of CsA across/into the corneal cells were evaluated using in vitro and ex vivo experiments. The cellularuptakewas investigated by replacing CsA with the fluorescent dye Rhodamine B. The penetration enhancement properties were supported by confocal laser scanning microscopy analysis. The internalization of SLNs in cornea and in RCE cell lines was confirmed, pointing out the possibility of CsA targeting to the cornea