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This work aimed to develop a new efficient approach for safe treatment of psoriasis. To achieve that, resveratrol-loaded spanlastics(F1-F12) were prepared and evaluated by complete in vitro characterization. The two optimal formulations (F10 and F11) had their particle size in the nano range with high entrapment efficiency and sustainable drug release. These two formulae were incorporated in carbopol 934 gel formulations (G1-G8) with different concentrations of drug and carbopol 934 polymer. G1 and G5 (1% w/w Carbopol 934 gel and 0.1% resveratrol) showed 40.13% ± 2.017% and 73.76% ± 2.46%,8 hours drug release, respectively. Their pH was accepted and non-irritant. At a shear stress of 500 s−1, G1 and G5 showed a reasonable viscosity of 1048.5 ± 2.12 cps and 954 ± 2.15 cps, respectively. In the in vivo psoriasis study, mice treated by G5 gel showed significant improvement of erythema and scaling compared to positive control group and they maintained healthy skin as shown in histopathological observations. Moreover, this group showed the least changes in mRNA expression of inflammatory cytokines. Concisely, our results suggest that selected carbopol gel of resveratrol-loaded spanlastics could maximize resveratrol topical anti-psoriatic effect.

Although there are several treatments for rheumatoid arthritis (RA), outcomes are unsatisfactory and often associated with many side effects. We attempted to improve RA therapeutic outcomes by intr...

Breast cancer endocrine resistance prevents unleashing full capabilities of Tamoxifen (TMX), besides TMX off-target side effects on healthy tissue. In this study, we engineered TMX nanocomposite via co-loading it on alginate-based silver nanoparticles and embedding within folic acid-polyethylene glycol surface conjugate. The coating process was done by w/o/w double emulsion method. To confirm the silver nanoparticles formation, UV spectroscopy, XRD and TEM analysis were carried out. TEM results confirmed the core-shell structure of folate targeted nanocomposite with approximate average diameter of 66 nm, the nanocomposite structures were characterized by FTIR, TGA and SEM. By comparing with the non-targeted formula, folate decorated formula had 12-folds lowered IC50 value and 12.5–14-fold higher cancer cells toxic selectivity index. Also, after 4 h treatment, both fluorescence microscopic and flow cytometric analysis indicated higher intracellular accumulation of folic acid conjugated formula on MCF-7 cancer cells than the non-targeted one with 3.44-folds. The breast cancer cytotoxic effects of this metal-endocrine nanocomposite formula could be explained by the induction of reactive oxygen species (ROS), down regulation of survival oncogenic genes (BCL-2 and Survivin) and the accumulation of MCF-7 cells in G2/M phase. All these data confirm the efficiency and efficacy of the formulated nanocomposite as future treatment for breast cancer.

The objective of this study was to improve effectiveness of resveratrol (RES) through brain targeting by the intranasal olfactory mucosa for the treatment Alzheimer’s disease (AD). To attain this, chitosan coated bilosomes (non ionic surfactant vesicles stabilized by bile salts, loaded with RES and superparamagnetic iron oxide nanoparticles (SPIONs) were prepared and incorporated into sodium alginate/PVP wafers. In vitro characterization of bilosomes including colloidal characteristics, entrapment efficiency and in vitro release was carried out. Hydration capacity, porosity percentage, morphology and in vitro release for selected wafer formulation were also investigated. Particle size of selected bilosomes, CS coated bilosome and SPION bilosomes was 208, 238 and 243 nm, respectively and they provided sustained RES release for 24 h. Both formulations were loaded in wafers and intra-nasally administered in mice with lipopolysaccharide induced AD model. Neurobehavioral tests, AD markers analysis, RT-PCR, western blotting and histopathological evaluation of the dissected brains were carried out. Results revealed the superiority of SPION bilosomes over conventional bilosomes and RES suspension in improving cognitive and memory functions, reduction of pro-inflammatory markers levels and down regulation of expression of NF-κB and P38. This may be attributed to enhanced RES therapeutic effects upon nanoencapsulation, loading into wafers, nasal administration and enhanced targeting the application of an external magnetic field.

This study was aiming to improve the effect of the water-insoluble drug, resveratrol, by encapsulating it in surfactant-based elastic vesicles (spanlastics). Spanlastics (SLs) were prepared by thin film hydration method using different ratios of Span 60 (S60) and edge activators (EAs). The prepared SLs were subjected to full

Systemic rheumatoid arthritis treatment has been associated with numerous side effects. We attempted to formulate hyaluronic acid (HA)-coated teriflunomide (TER)-loaded nanostructured lipid carriers (NLCs) that can target inflamed rheumatic joints following oral administration. In vitro evaluation including colloidal characteristics, drug release and stability studies were conducted. Also, cytotoxicity studies on THP1 and peripheral blood mononuclear cells besides testing the binding of HA coated TER-NLCs to CD44 receptors were carried out. Furthermore, pharmacokinetics following oral administration, anti-arthritic effects, hepato and nephrotoxicity of NLCs were assessed. Selected NLCs formulation was approximately 284.9 ± 3.8 nm in size with 96.89 ± 0.45% entrapment efficiency and provided a sustained release for 30 days. NLCs showed good stability that was confirmed by TEM examination. Cell culture studies revealed that HA-coated TER- NLCs showed superior cytotoxicity and binding affinity to CD44 receptors compared with TER suspension. In vivo studies demonstrated the superiority of NLCs in increasing TER bioavailability, reducing TNF-α serum levels and improving joint healing that was evidenced in both histopathological and X-ray radiographic examination. This may be attributed to the ability of HA-coated TER-NLCs to target rheumatic joints passively and actively by targeting CD44 receptors that are overexpressed in rheumatic joints.

Although there are several treatments for rheumatoid arthritis (RA), outcomes are unsatisfactory and often associated with many side effects. We attempted to improve RA therapeutic outcomes by intra-articular administration of dual drug-loaded poly(lactic) acid (PLA)-coated herbal colloidal carriers (HCCs). Curcumin (CU) and resveratrol (RES) were loaded into HCCs because of their safety and significant anti-inflammatory activity. HCCs were prepared using a high-pressure, hot homogenization technique and evaluated

The present study improved the effectiveness of a poorly water-soluble drug, luteolin (LUT), by encapsulating it in lecithin-bile salt-integrated system called bilosomes (BLs). Such a delivery system offers the benefits of mimicking the skin's biological structure and being a prominent tool to circumvent skin delivery obstacles. The prepared BLs underwent complete in vitro assessment. The developed BLs showed enhanced characteristics compared to free luteolin suspension (P 0.05). Optimized BLs attained good entrapment efficiency (78.60% ± 0.88%), small particle size (226.1 ± 2.45 nm), and sustained drug-release pattern. The study also showed that both blank and LUT-loaded BLs preparations were safe to the skin with a primary irritancy index of 2 based on the Draize test. In vivo tests were conducted to study the effect of the bile salt-based nanovesicles compared with the free LUT suspension. The photoprotective effect was evaluated according to the visual examination and biochemical analyses of antioxidant, anti-inflammatory, and anti-wrinkling markers after ultraviolet B irradiation. Results of biochemical markers and histopathological examination demonstrated that the LUT-BLs effect was superior than the LUT suspension (P 0.05). Consequently, the current study proves that novel LUT-loaded BLs is a promising nanoplatform that overcome LUT delivery obstacles and, hence, alleviate UV-induced skin damage.

The study aims to elaborate novel self-assembled liquid crystalline nanoparticles (LCNPs) of resveratrol which has neuro-protective, anti-aging, and anticancer activity. Resveratrol loaded LCNPs fabrication and optimization for transdermal delivery was assessed via a quality by design approach based on 2

The objective of the study was to target clonazepam to the brain through the intranasal olfactory mucosa using nanolipid carriers loaded with superparamagnetic iron oxide nanoparticles (SPIONs) to allow nanocarrier guidance and retention with an external magnetic field. For improved delivery, the nanolipid carriers were incorporated in a thermosensitive mucoadhesive in situ gel. Different nanolipid carriers including solid lipid nanoparticles and nanostructured lipid carriers (NLC) were prepared and characterized with respect to particle size, zeta potential, entrapment efficiency, and in vitro release. The NLC composed of 3 solid lipids (Compritol ® 888, stearic acid, and glyceryl monostearate) and 2 liquid oils (oleic acid and glyceryl monooleate) showed the most satisfactory characteristics and was loaded with SPION (NLC/SPION). Both formulae (NLC and NLC/SPION) were incorporated in an optimized thermosensitive mucoadhesive in situ system composed of 15% pluronic 127 and 0.75% sodium alginate and evaluated for the anticonvulsant action in chemically induced convulsive Swiss Albino mice. The treatment of animals with NLC/SPION significantly prolonged the onset times for convulsion and considerably protected the animals from death. One can thus hope for the emergence of a new intranasal treatment of epilepsy with consequent decrease in peripheral side effects of clonazepam.

Citalopram HCl (CH) is one of the few drugs which can be used safely in childhood psychiatric disorders. This study was focused on the preparation of interpenetrating polyelectrolytes nano-complexes (IPNC) to transform the hydrophilic carbohydrate polymers into an insoluble form. The IPNCs were loaded with CH to sustain its effect. The IPNC2 (composed of chitosan:pectin in a 3:1 ratio) showed the most extended drug release pattern (P

The advantages of multiparticulate carriers over monolithic one are well known. In this study, mucoadhesive micropellets (MPs) composed of metronidazole (MTZ)–polysaccharide(s) polyelectrolytes com...

Solar irradiation induces skin inflammatory processes causing deleterious effects like premature ageing. In this study, the designed lipoid colloidal carrier (LCC) was loaded with Diosmin in combination with different essential oils, to be used as a topical photo-protective preparation. To investigate the ability of the essential oils to potentiate Diosmin effects, the Diosmin/essential oil-loaded LCCs (LCC2, LCC3 and LCC4) were compared to the Diosmin-loaded LCC (LCC1). The incorporated essential oils were those of Rosmarinus officinalis, Zingiber officinale or Vitis vinifera in LCC2, LCC3 and LCC4, respectively. All the LCCs had particle size (PS) values ranging from 121.1 to 144.3nm with uniform distribution and, zeta potential (Z) values around 30mV. Also, they all had high drug encapsulation efficiencies. LCC1 had the lowest anti-oxidant and in-vitro sun-blocking effect (p

Arthritis is a chronic degenerative joint disease decreasing the patient's quality of life. Mixed micellar system (MM) was exploited as a nanotechnology platform suitable for the encapsulation of the water-insoluble drug, Resveratrol (RES). MM were prepared using different ratios of poloxamer 188 (P188) and poloxamer 407 (P407), and then subjected to in-vitro evaluation. The selected MM (MM3) composed of P188: P407 in a ratio of 2:1 attained the most compromised properties (Particle size = 52.97 ± 4.52 nm, Encapsulation Efficiency = 76.20 ± 4.51 and Release efficiency = 76.26 ± 6.25), and was coated with poly-lactic acid (PLA). TEM photographs of PLA-coated MM3 showed a polymeric layer surrounding the nanoparticles. Rats with induced arthritis were used to study the curative effect of intra-articularly (IA)-injected MM3, PLA-coated MM3 as well as the drug suspension. All the treated groups showed a significant therapeutic improvement in arthritis proved by measuring rats knee diameter as well as the tumor necrosis factor-alpha (TNF-α). The treatment effectiveness was in the following order: PLA-coated MM3 ˃ MM3 ˃ drug suspension, (p 0.05). Histological study showed the recovery of the joints and synovial structure by IA administration of the drug-loaded micellar nanosystems, and the PLA-coated MM attained the best effect. This study proves the promising curative effect of the designed nanotechnology-based drug carrier.

In this study, Compritol ATO-based Resveratrol colloidal carriers (CCCs) were prepared and subjected to characterization and evaluation. In most formulae, the use of a binary-mixture of surfactants improved the physicochemical properties. CCC6 (containing P407/P188 as bi-surfactants) attained the highest drug loading, release efficiency during 24 h and occlusive effect for 48 h; in addition, it showed a uniform particle size distribution within the desired range. In-vivo studies were done based on the analysis of anti-oxidant markers [catalase (CAT), reduced glutathione (GSH) and superoxide dismutase (SOD)], anti-inflammatory markers [interleukin 6 (IL-6), interleukin 8 (IL-8) and rat Nuclear factor-kappa B (NF-κB)] and anti-wrinkling markers [matrix metalloproteinase (MMP-1) and Granulocyte-macrophage colony-stimulating factor (GM-CSF)], after UVB-irradiation. Results were significantly different when comparing the positive control and the negative control groups (p 0.05). Rats pre-treated with CCC6 showed a great amelioration, and the level of the biochemical markers was significantly different compared to those of the positive control group and those pre-treated with the drug suspension (p 0.05). Also, the high skin protective effect of CCC6 was proved by visual and histopathological examination of the rats' skin. Therefore, the current study proves the beneficial effects of the designed dermal Resveratrol-loaded colloidal system.

To avoid frequent drug administration, PLGA-based monolithic filament-shaped implants were prepared. In this study, the effect of different formulation variables was studied, namely: type of PLGA (PLGA 502 and PLGA 503), type of drug (the lipophilic Prednisolone acetate, PA and the hydrophilic Propranolol Hydrochloride, PH) and drug loading (10 and 30% w/w). PLGA 503-based implants showed a lower water uptake, lower mass loss and erosion, slower drug release, and better mechanical properties and elasticity (P

Objective: Coconut oil (CO) was used in combination with metronidazole in order to prepare vaginal pessaries ameliorating the use, delivery and efficacy of the anti-mycotic treatment.Methods: To prepare the metronidazole–loaded pessaries, different lipids, namely: suppocire NA15 (SNA), suppocire NAIS10 (SIS), suppocire AM (SAM) and ovucire WL 2944 (OWL) were used alone or in combination with coconut oil in a ratio of 1:1. Prepared pessaries were subjected to characterization and evaluation of physical properties, drug release, anti-microbial effect, in vivo studies and histopathological examination.Results: In the case of all the lipids, coconut oil improved the physical properties which can allow better use and performance of the pessaries. Among the prepared pessaries, the OWL/CO-based pessary (P8) showed the highest drug release profile (P