Chondroitin sulphate mediated targeted delivery of methotrexate and aceclofenac to the joints for effective management of rheumatoid arthritis

Development and Optimization of Teriflunomide-Loaded Chondroitin Sulphate-Coated Nanostructured Lipid Carriers (Nlcs) Through Box Behnken Design

“…As observed in other NLC-based formulations elaborated with similar components [51,56,57] the release profile for NLC-TFM is biphasic, with a burst effect that released approximately 30% of TFM within the 4 first hours, followed by a sustained release until 72 h. In the case of CHS-NLC-TFM, the release of drug is slower than the observed on NLC-TFM, suggesting the ability of CHS to form an outer layer capable of retaining the TFM located at the surface of the NLC. This feature has been evidenced in previous studies [21] In comparison to other nanoparticulated release systems including NLCs loaded with TFM, our formulations show a slightly more sustained release of the drug over time [28,58,59]. The release of TFM as free drug was fast, reaching a 98.45% in 12 h. In contrast, the sustained release of TFM after 12 h could be attributed to the phospholipid/Compritol lipidic barrier, [24] which restricts the penetration of aqueous medium into the Compritol-lecithin-triolein core and reduces the mobilization of TFM, prolonging its release over time [48]…”

“…The presented findings suggest that the TFM is properly encapsulated within NLCs, but the addition of CHS has a negative impact on EE%, an effect that can be relatively reduced by adjusting the load of TFM and CHS to find an ideal ratio. This outcome has been previously reported [12,15,21,44] and could be explained by the leaching of TFM from the NLCs, due to the increased time necessary to coat with the CHS solution [46] . Other reported mechanisms are the competitive behavior of TFM and CHS to interact with the hydrophobic sites of lecithin and lipidic components of NLCs.…”

“…[18] Drug-loaded lipid nanoparticles (SLNs and NLCs) can be customized for targeted drug delivery with glycosaminoglycans such as chondroitin sulfate (CHS). [12,19] CHS can actively target affected joints through selective binding to CD44 receptors overexpressed in RA [20]promoting accumulation and retention of the drug in the synovial tissue while minimizing side effects and dosage [21] Although NLCs have been widely studied as drug delivery systems (DDS), the outcomes associated to the factors involved in their formulation are not always predictable. To address this issue, statistical tools systematize the experimental design and optimize the pre-formulation process, since there is a more detailed analysis of the influence of each factor in the outcome.…”

Dermal Delivery of Docetaxel Loaded Nano Liquid Crystals for the Treatment of Skin Cancer

“…It was observed that the percent drug entrapment was decreasing with increasing the concentration of surfactant and on increasing the time of sonication. It is due to the extract out the drug from particles on increasing the mechanical force by sonication and size reduction of size NLCs on increasing the concentration of surfactant due to their surfactant action [16,[23][24][25][26]. Stability study data was revealed that the optimized formulation stable after 3 mo of storage at 4ᵒC while at 25-28±2 °C, the formulation was found unstable.…”

CD44 receptor-targeted novel drug delivery strategies for rheumatoid arthritis therapy

“…Chondroitin sulfate (CS) is a water-soluble, unbranched sulfated anionic glycosaminoglycan composed of alternating 4-linked β-d-glucuronic acid, and 3-linked N-acetyl galactosamine disaccharide units with varied sulfate positions [12]. The sulfate group imparts hydrophilicity, and was found on the fourth and sixth positions in CS, which are named CS A and CS C, respectively.…”