Novel self-assembled tacrolimus nanoparticles cross-linking thermosensitive hydrogels for local rheumatoid arthritis therapy

Wu, Huimin; Wang, Kaiyuan; Wang, Hanning; Chen, Fang; Huang, Wencong; Chen, Yuqi; Chen, Jiali; Jin, Tao; Wen, Xiaoguang; Xiong, Sheng

doi:10.1016/j.colsurfb.2016.10.013

Cited by 46 publications

(41 citation statements)

References 36 publications

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“…It has a low critical micelle concentration (CMC) and its micelles are highly stable after dilution [ 34 , 35 ]. It is an innovative excipient that gives new levels of solubility and bioavailability of poorly water-soluble drugs and natural compounds both for oral and parenteral administration [ 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 ]. Solutol ® HS15 (polyoxyethylene esters of 12-hydroxystearic acid, Figure 2 ) is a known non-ionic surfactant with high solubility and stability and low toxicity in vivo.…”

Section: Introductionmentioning

confidence: 99%

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Bergonzi

Vasarri²,

Marroncini

et al. 2020

Molecules

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Thymoquinone (TQ) is the main active ingredient of Nigella sativa essential oil, with remarkable anti-neoplastic activities with anti-invasive and anti-migratory abilities on a variety of cancer cell lines. However, its poor water solubility, high instability in aqueous solution and pharmacokinetic drawbacks limits its use in therapy. Soluplus® and Solutol® HS15 were employed as amphiphilic polymers for developing polymeric micelles (SSM). Chemical and physical characterization studies of micelles are reported, in terms of size, homogeneity, zeta potential, critical micelle concentration (CMC), cloud point, encapsulation efficiency (EE%), load capacity (DL), in vitro release, and stability. This study reports for the first time the anti-migratory activity of TQ and TQ loaded in SSM (TQ-SSM) in the SH-SY5Y human neuroblastoma cell line. The inhibitory effect was assessed by the wound-healing assay and compared with that of the unformulated TQ. The optimal TQ-SSM were provided with small size (56.71 ± 1.41 nm) and spherical shape at ratio of 1:4 (Soluplus:Solutol HS15), thus increasing the solubility of about 10-fold in water. The entrapment efficiency and drug loading were 92.4 ± 1.6% and 4.68 ± 0.12, respectively, and the colloidal dispersion are stable during storage for a period of 40 days. The TQ-SSM were also lyophilized to obtain a more workable product and with increased stability. In vitro release study indicated a prolonged release of TQ. In conclusion, the formulation of TQ into SSM allows a bio-enhancement of TQ anti-migration activity, suggesting that TQ-SSM is a better candidate than unformulated TQ to inhibit human SH-SY5Y neuroblastoma cell migration.

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Section: Introductionmentioning

confidence: 99%

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Bergonzi

Vasarri²,

Marroncini

et al. 2020

Molecules

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“…Other applications described the use of Soluplus for doxorubicin delivery in the treatment of resistant tumors [20] or to increase acyclovir permeability across the cornea and sclera [22] or even to enhance oral bioavailability and hypouricemic activity of scopoletin [23]. Numerous other applications are described in the literature [24][25][26][27].…”

Section: Introductionmentioning

confidence: 99%

“…Considering the high migratory and metastatic capacity of neuroblastoma, it is possible to exploit new therapies loaded in nanocarriers to improve the drug efficacy in order to counteract these specific neuroblastoma abilities. Nanoformulations can also be used for the delivery of molecules of natural origin or phytocomplexes to optimize the effectiveness of herbal medicines [13,20,27]. In this perspective, the possibility of using the whole crude extract carried by nanocarriers leads to having better biological efficacy due to the synergistic action of the bioactive compounds of the phytocomplex with respect to the activity of the single compounds.…”

Section: Introductionmentioning

confidence: 99%

Comparison of Chitosan Nanoparticles and Soluplus Micelles to Optimize the Bioactivity of Posidonia oceanica Extract on Human Neuroblastoma Cell Migration

et al. 2019

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Posidonia oceanica (L.) Delile is a marine plant endemic of Mediterranean Sea endowed with interesting bioactivities. The hydroalcholic extract of P. oceanica leaves (POE), rich in polyphenols and carbohydrates, has been shown to inhibit human cancer cell migration. Neuroblastoma is a common childhood extracranial solid tumor with high rate of invasiveness. Novel therapeutics loaded into nanocarriers may be used to target the migratory and metastatic ability of neuroblastoma. Our goal was to improve both the aqueous solubility of POE and its inhibitory effect on cancer cell migration. Methods: Chitosan nanoparticles (NP) and Soluplus polymeric micelles (PM) loaded with POE have been developed. Nanoformulations were chemically and physically defined and characterized. In vitro release studies were also performed. Finally, the inhibitory effect of both nanoformulations was tested on SH-SY5Y cell migration by wound healing assay and compared to that of unformulated POE. Results: Both nanoformulations showed excellent physical and chemical stability during storage, and enhanced the solubility of POE. PM-POE improved the inhibitory effect of POE on cell migration probably due to the high encapsulation efficiency and the prolonged release of the extract. Conclusions: For the first time, a phytocomplex of marine origin, i.e., P. oceanica extract, has enhanced in terms of acqueous solubility and bioactivity once encapsulated inside nanomicelles.

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“…10 Via direct injection into the affected joints, DLTH can not only achieve drug enrichment at target morbid joints and minimize systemic toxicity, but also prolong release duration time and reduce burst drug release, leading to improved Dex therapeutic index and less risks of adverse effects. 11 Collagen-induced arthritis (CIA), is one of the most widely adopted animal models that shares similar clinical and histopathologic characteristics as that of human RA, such as swelling, pain, synovial hyperplasia, deformity in affected joints. 4 Hence, it is an ideal model to illustrate the anti-inflammatory and pain-relieving effects of DLTH joint injection in studies of RA inflammation and RA-related pain research, and we aimed to explore the underlying mechanisms of DLTH in anti-inflammatory activity and effective pain relief.…”

Section: Introductionmentioning

confidence: 99%

<p>Dexamethasone-Loaded Thermosensitive Hydrogel Suppresses Inflammation and Pain in Collagen-Induced Arthritis Rats</p>

Wang¹,

Xu²,

Fan³

et al. 2020

DDDT

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To overcome negative adverse effects and improve therapeutic index of dexamethasone (Dex) in rheumatoid arthritis (RA), we developed a novel sustained release formulation-intra-articular injectable dexamethasone-loaded thermosensitive hydrogel (DLTH) with chitosan-glycerin-borax as carrier for the remission of inflammation and pain. The focus of this article is to explore both anti-inflammatory and pain-relieving effects of DLTH joint injection in bovine type-II collagen-induced arthritis (CIA) rats. Methods: Wistar rats were randomized into three groups, including the normal group (n=6), the model group (n=6) and the DLTH group (n=10). Joint injection of DLTH (1mg/kg Dex per rat) was injected on day 12 in the DLTH group twice a week for three weeks. Clinical signs of body weight, paw swelling and arthritis scores, histologic analysis, hind paw mechanical withdrawal threshold (MWT), plantar pressure pain threshold (PPT) were taken into consideration. Serum contents of IL-17A, prostaglandin E2 (PGE2), prostacyclin 2 (PGI2) and prostaglandin D2 (PGD2), real-time polymerase chain reaction (PCR) analysis of inflammatory factors and pain-related mediators in synovium and dorsal root ganglia (DRG), Western blotting of NF-κB in synovium were all evaluated. Results: Paw swelling, arthritis scores and joint inflammation destruction were all attenuated in the DLTH-treated group. Results showed that DLTH not only down-regulated serum IL-17A, but also mRNA levels of inflammatory factors and NGF, and key proteins contents of the NF-κB pathway in synovium. Increases of MWT and PPT in DLTH-treated rats elucidated pain-reducing effects of DLTH. Elevated serum PGD2 levels and declines of serum PGE2 and PGI2, and inflammatory and pain-related genes in DRGs in the DLTH group were also recorded. Conclusion: These data elucidated that DLTH joint injection impeded synovial inflammation processes through down-regulating transcription activity of NF-κB pathway, and intraarticular DLTH may aid in the regulation of RA pain through regulating inflammation and pain conduction process.

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Novel self-assembled tacrolimus nanoparticles cross-linking thermosensitive hydrogels for local rheumatoid arthritis therapy

Cited by 46 publications

References 36 publications

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Thymoquinone-Loaded Soluplus®-Solutol® HS15 Mixed Micelles: Preparation, In Vitro Characterization, and Effect on the SH-SY5Y Cell Migration

Comparison of Chitosan Nanoparticles and Soluplus Micelles to Optimize the Bioactivity of Posidonia oceanica Extract on Human Neuroblastoma Cell Migration

<p>Dexamethasone-Loaded Thermosensitive Hydrogel Suppresses Inflammation and Pain in Collagen-Induced Arthritis Rats</p>

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