Novel rhein–phospholipid complex targeting skin diseases: development, in vitro, ex vivo, and in vivo studies

Ebada, Heba M K; Nasra, Maha M A; Elnaggar, Yosra S.R.; Abdallah, Ossama Y.

doi:10.1007/s13346-020-00833-1

Cited by 26 publications

(13 citation statements)

References 69 publications

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“…For example, Li et al found that HPDM-rhein can cross the blood-pancreatic barrier and specifically aggregate in the lungs, thereby improving acute lung damage caused by pancreatitis (AP) [ 109 ]. And rhein-phospholipid complex (RH-PLC) improves the solubility and skin permeability of rhein [ 110 ]. Multiple substitutions at other sites can enhance pharmacological activity, such as enhancing antitumor activity [ 111 , 112 ] and antibacterial [ 113 ].…”

Section: Conclusion and Discussionmentioning

confidence: 99%

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Chen

Zhang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Rhein, belonging to anthraquinone compounds, is one of the main active components of rhubarb and Polygonum multiflorum. Rhein has a variety of pharmacological effects, such as cardiocerebral protective effect, hepatoprotective effect, nephroprotective effect, anti-inflammation effect, antitumor effect, antidiabetic effect, and others. The mechanism is interrelated and complex, referring to NF-κB, PI3K/Akt/MAPK, p53, mitochondrial-mediated signaling pathway, oxidative stress signaling pathway, and so on. However, to some extent, its clinical application is limited by its poor water solubility and low bioavailability. Even more, rhein has potential liver and kidney toxicity. Therefore, in this paper, the pharmacological effects of rhein and its mechanism, pharmacokinetics, and safety studies were reviewed, in order to provide reference for the development and application of rhein.

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Section: Conclusion and Discussionmentioning

confidence: 99%

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Chen

Zhang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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“…CHS-CA-NRs morphology was assessed compared to non-functionalized CA-NRs using TEM (JEM-100S, JOEL Ltd, Japan) after uranyl acetate staining on a carbon- laminated copper grid (Ebada et al. 2021 ).…”

Section: Methodsmentioning

confidence: 99%

“…The inherent fluorescence attributes of CA (Ebada et al. 2021 , 2021 ) was exploited to determine the residence time and to assess the cartilage-targeting ability of different intra-articular CA-NRs. Fluorescence was quantified in cartilage sections at different intervals in healthy or arthritic knee joints following previous report with some modifications (Sacchetti et al.…”

Section: Methodsmentioning

confidence: 99%

Chondroitin sulfate-functionalized lipid nanoreservoirs: a novel cartilage-targeting approach for intra-articular delivery of cassic acid for osteoarthritis treatment

et al. 2022

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Novel intra-articular nanoreservoirs were implemented employing different cartilage targeting approaches to improve cartilage bioavailability of a chondroprotective drug, cassic acid (CA), for effective amelioration of cartilage deterioration off-targeting CA gastrointestinal disorders. Herein, we compared active cartilage-targeting approach via chondroitin sulfate (CHS) functionalization versus passive targeting using positively charged nanoparticles to target negatively charged cartilage matrix. Firstly, CA integrated nanoreservoirs (CA-NRs) were fabricated based on ionic conjugation between CA and cationic hydrophobic surface modifier octadecylamine (ODA) and were further functionalized with CHS to develop CHS-CA-NRs. Confocal laser microscope was used to visualize the accumulation of nanoparticles into the cartilage tissue. Both targeting approaches promoted CA local cartilage availability and prolonged its residence time. Compared to passive targeted CA-NRs, active targeted CHS-CA-NRs showed higher fluorescence signals in proximity to and inside chondrocytes which lasted for up to 21 days. In MIA-osteoarthritic rats, CHS-CA-NRs showed superior antiosteoarthritic activity, exhibiting highest cartilage repair compared to CA-NRs. Additionally, CHS-CA-NRs significantly inhibited OA inflammatory cytokine, degradation enzyme and oxidative stress and improved cartilage matrix biosynthesis. Conclusively, CHS-CA-NRs improved OA repair showing a superior efficacy for articular cartilage targeting with CHS which could be a potential advance for OA therapy.

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“…On the other hand, due to its amorphous nature, PL diffractogram showed a single broad peak at 20°. 47 Whereas the diffraction pattern of the physical mixture retained both the characteristic crystalline peaks of Fas and the broad peaks of PL, the crystalline peaks disappeared in the case of Fas/ PL complex indicating a change in the physicochemical properties of Fas suggesting successful complex formation with PL.…”

Section: X-ray Diffraction (Xrd)mentioning

confidence: 96%

“…Phospholipid spectrum exhibited a band between 2925 and 2854 cm −1 corresponding to CH 2 , a band at 1736 cm −1 due to C=O stretching, P-O asymmetric and symmetric vibration bands at 1243 cm −1 and 1090 cm −1 , respectively, and a band at 969 cm −1 corresponding to N + (CH 3 ) 3 stretching. 47 Fas/Pl physical mixture showed comparative spectral analysis with no shift in the absorption peaks of either the drug or the phospholipid. On the other hand, the proposed complex FTIR chart showed significant changes in many peaks.…”

Section: Physicochemical Characterization Of Fas/ Plmentioning

confidence: 99%

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

Khallaf¹,

El‐Moslemany²,

Ahmed

et al. 2022

IJN

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Purpose: Fasudil hydrochloride (Fas), a rho-associated protein kinase inhibitor, proved to be promising for glaucoma management owing to its IOP lowering and antioxidant effects. However, its highly hydrophilic nature limits ocular permeation and bioavailability. Hence, the study objective was the development of Fas loaded vesicular system with high entrapment efficiency formulated as a thermosensitive gel for local administration aiming to enhance ocular retention and permeation and hence therapeutic efficacy. Methods: Fasudil complex with phospholipid (Fas/PL) was prepared by solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). Fas/PL was further formulated as liposomes by methanol injection method and characterized regarding colloidal properties, entrapment efficiency (EE%) and in vitro drug release. The prepared liposomes were incorporated into an optimized thermosensitive in situ gel (Fas/PL-Lipo P407/HPMCgel ) selected based on gelling time and temperature and rheological properties. The effect of incorporation into gel on the in vitro characteristics of liposomes was investigated. The in vitro mucoadhesive potential, ex vivo permeation, irritability and efficacy in a glaucoma rabbit model were also assessed. Results: FT-IR and XRD suggested interactions between Fas and PL, proposing complexation. Fas/PL liposomal dispersions showed good colloidal properties (particle size: 132.5 ± 1.6 nm, zeta potential: −21.6 ± 0.9 and %EE 78.6 ± 0.3%) with sustained drug release. In situ thermosensitive gel (20% poloxamer 407 and 0.5% HPMC) showed optimum gelling properties. The selected gel formulation reduced burst release of the drug, enhanced mucoadhesive properties and prolonged corneal permeation ex vivo. HET-CAM test confirmed that the prepared formulations were non-irritant. In vivo pharmacodynamic study indicated improved bioavailability and significantly lower intraocular pressure (IOP) of Fas/PL-Lipo P407/HPMC gel compared to drug solution and liposomal dispersion. Conclusion:The results present Fas/PL-Lipo P407/HPMC gel as a potential platform for ophthalmic delivery of fasudil with improved pharmaceutical attributes and enhanced bioavailability and efficacy in glaucoma.

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Novel rhein–phospholipid complex targeting skin diseases: development, in vitro, ex vivo, and in vivo studies

Cited by 26 publications

References 69 publications

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Update on Pharmacological Activities, Security, and Pharmacokinetics of Rhein

Chondroitin sulfate-functionalized lipid nanoreservoirs: a novel cartilage-targeting approach for intra-articular delivery of cassic acid for osteoarthritis treatment

Exploring a Novel Fasudil-Phospholipid Complex Formulated as Liposomal Thermosensitive in situ Gel for Glaucoma

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