Core–shell structured gel-nanocarriers for sustained drug release and enhanced antitumor effect

He, Wei; Lv, Yaqi; Zhao, Yaping; Xu, Chaoran; Zhu, Jin; Qin, Chao; Yin, Lifang

doi:10.1016/j.ijpharm.2015.02.053

Cited by 25 publications

(18 citation statements)

References 42 publications

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“…The CM-Ns were prepared using a high-pressure homogenization method as described in a previous report. 15 Briefly, 100 mg of CM and 300 mg of Solutol-HS 15 were dissolved in 200 mL of soybean oil. The oil phase was then mixed with 20 mL of water using a high speed electric disperser (FS-2, Huier Co. Ltd., Hangzhou, People’s Republic of China) to form a coarse emulsion.…”

Section: Methodsmentioning

confidence: 99%

The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats

Zheng¹,

Sun²,

Liu³

et al. 2015

DDDT

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BackgroundRheumatoid arthritis (RA), induced by the prolonged inappropriate inflammatory responses, is one of the most prevalent of all chronic inflammatory joint diseases. Curcumin (CM), a yellow hydrophobic polyphenol derived from the herb turmeric, has various pharmacological activities against many chronic diseases and acts by inhibiting cell proliferation and metastasis and downregulating various factors, including nuclear factor kappa B, interleukin-1β and TNF-α. Given the pathogenesis of RA, we hypothesized that the drug also has antiarthritic effects. The aims of the present study included the following: 1) examining the therapeutic effect of CM administered via intravenous (iv) injection on RA and 2) formulating the drug into oil–water nanoemulsions (Ns) to overcome the low oral bioavailability of CM and achieve oral delivery of the drug.MethodsThe effect of CM administered through iv injection on adjuvant-induced arthritis in rats was studied in terms of paw swelling, weight indices of the thymus and spleen, and pathological changes in nuclear factor kappa B expression and inflammatory cytokines. Methotrexate was used as a positive control. The CM-Ns were prepared using a high-pressure homogenizing method and characterized with respect to the particle size and morphology. The stability of the CM-Ns in simulated gastrointestinal (GI) fluids and in vitro release were also investigated. A pharmacokinetic study of the CM-Ns and suspensions in which the plasma levels were determined using an high performance liquid chromatography method and the pharmacokinetic parameters were calculated based on a statistical moment theory was also performed in rats.ResultsCM administered via iv injection had a therapeutic effect on RA similar to methotrexate. CM-Ns with a diameter of approximately 150 nm were successfully prepared, and the drug was well encapsulated into the Ns without degradation in simulated GI conditions. The area under the curve (AUC) and Cmax for the CM-Ns were more than threefold greater than those for the suspensions; moreover, similar decreases in the levels of TNF-α and interleukin-1β in both synovial fluid and blood serum were obtained from oral administration of CM-Ns and iv injection.ConclusionCM was an effective antiarthritic agent, and the present N formulation appeared to be a promising system that allowed RA therapy with CM to be converted from iv to oral administration.

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Section: Methodsmentioning

confidence: 99%

The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats

Zheng¹,

Sun²,

Liu³

et al. 2015

DDDT

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“…To study the drug state in ANSs, examinations of PXRD and DSC were performed. Pure PTX displayed characteristic crystal peaks at a 2θ angle of 5.0, 9.0, 10.0 and 12.0 [ 26 ], demonstrating high crystallinity ( Figure 3 A). Similar crystalline peaks were displayed in the physical mixture (PM).…”

Section: Resultsmentioning

confidence: 99%

Amorphous Nanosuspensions Aggregated from Paclitaxel–Hemoglobulin Complexes with Enhanced Cytotoxicity

et al. 2018

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Amorphous nanosuspensions (ANSs) enable rapid release and improved delivery of a poorly water-soluble drug; however, their preparation is challenging. Here, using hemoglobin (Hb) as a carrier, ANSs aggregated from paclitaxel (PTX)–Hb complexes were prepared to improve delivery of the hydrophobic anti-cancer agent. An affinity study demonstrated strong interaction between Hb and PTX. Importantly, the complexes could aggregate into <300 nm ANSs with high drug loading, which acidic condition facilitated their formation. Furthermore, the ANSs possessed improved cytotoxicity against cancer cells over the crystalline nanosuspensions. Taken together, ANSs aggregated from PTX–Hb complexes were developed, which could kill cancer cells with high efficiency.

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“…12‐Hydroxystearic acid (HSA) is one of these LMWGs used as a gelator for cooking oils . In addition, a supramolecular organogel made from HSA has been actively investigated for bioapplications, cosmetics and as a xerogel for recovery of oil spills . HSA is able to gel various organic solvent such as paraffin oil, octyl palmitate, and silicone oil by the formation of interconnected crystalline fibers .…”

Section: Introductionmentioning

confidence: 99%

A Supramolecular Gel Based on 12‐Hydroxystearic Acid/Virgin Coconut Oil for Injectable Drug Delivery

Tantishaiyakul

Ouiyangkul

Wajasat

et al. 2018

Euro J Lipid Sci & Tech

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A supramolecular organogel based on 3 wt% of 12‐hydroxystearic acid (HSA) and virgin coconut oil (oil) in the presence of a gel inhibitor, 4 wt% ethanol (EtOH), is developed and investigated for injectable implant delivery. Gel formation is observed by the test tube tilting method. The characteristic properties of the sol‐gel system are determined using rheological, thermal, and turbidity analyses. The in vitro releases of piroxicam (PX) and diclofenac acid (DFA), the models for hydrophilic and lipophilic drugs, respectively, are performed. Characterization of the blends from the three methods are comparable and indicate that the systems of HSA/oil, PX/HSA/oil, and DFA/HSA/oil gel at about 36–39 °C upon cooling and the gel turns to a sol at a temperature higher than 50 °C upon heating at a rate of 2 °C min−1. Isothermal measurements reveals that HSA/EtOH/oil, PX/HSA/EtOH/oil, and DFA/HSA/EtOH/oil remain as a sol for about 18 min at room temperature (25 °C). Both PX and DFA show a sustained release from HSA/oil and HSA/EtOH/oil. Practical Applications: The presence of ethanol which is a hydrophilic molecule can disrupt the interaction between HSA molecules and suppress gel formation at the low temperature that the system normally forms gel. This HSA/EtOH/oil system might be injectable at room temperature and become gels at the site of injection when EtOH is diffused to other tissues in the body. This system is beneficial for use as an injectable implant system for a sustained delivery of both hydrophilic and hydrophobic drugs. 12‐hydroxystearic acid (HSA) and virgin coconut oil (oil) can form gels at body and lower temperatures e.g., room temperatures. The sol‐gel system is characterized using rheological, thermal, and turbidity methods. Ethanol inhibits gel formation at room temperature to facilitate injection. The mixture of HSA, ethanol, and oil might be used as an injectable implantation. Two hydrophobic (diclofenac) and hydrophilic (piroxicam) model drugs show sustained releases from HSA/oil and HSA/ethanol/oil.

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Core–shell structured gel-nanocarriers for sustained drug release and enhanced antitumor effect

Cited by 25 publications

References 42 publications

The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats

The effect of curcumin and its nanoformulation on adjuvant-induced arthritis in rats

Amorphous Nanosuspensions Aggregated from Paclitaxel–Hemoglobulin Complexes with Enhanced Cytotoxicity

A Supramolecular Gel Based on 12‐Hydroxystearic Acid/Virgin Coconut Oil for Injectable Drug Delivery

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