Studies of the Solubility of Rutin from Solid Dispersions

Ковальский, Иван Васильевич; Krasnyuk, I. I.; Nikulina, O. I.; Belyatskaya, A. V.; Kharitonov, Yu. Ya.; Feldman, Nataliya B.; Луценко, С. В.; Grikh, V. V.

doi:10.1007/s11094-014-1020-z

Cited by 8 publications

(3 citation statements)

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“…To check for irritation of the mucous membrane, a HET-CAM test (chorioallantoic membrane test) was carried out [ 51 ]. The essence of the method is as follows: Embryonated chicken eggs weighing 50.0–60.0 g without defects are incubated at a temperature of 37 ± 0.5 °C for 3 days and periodically turned over.…”

Section: Methodsmentioning

confidence: 99%

Thermosensitive Intravitreal In Situ Implant of Cefuroxime Based on Poloxamer 407 and Hyaluronic Acid

Bakhrushina,

Dubova,

Nikonenko

et al. 2023

Gels

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The main method of treatment and prevention of endophthalmitis is a combination of intravitreal and topical administration of antibiotics, such as cefuroxime moxifloxacin or vancomycin. However, this method is ineffective due to the rapid elimination of the drug. This problem can be solved with the help of intravitreal in situ injection systems, which are injected with a syringe into the vitreous body and provide prolonged action of the drug at the focus of inflammation. Under the influence of temperature, the liquid drug undergoes a phase transition and turns into a gel after injection. This ensures its prolonged action. The study aimed to develop an intravitreal in situ cefuroxime delivery system for the treatment of endophthalmitis based on a thermosensitive biodegradable composition of poloxamer 407 and hyaluronic acid. A combination of poloxamer Kolliphor® P407, Kolliphor® P188, and PrincipHYAL® hyaluronic acids of different molecular weights was used as a delivery system. The potency of cefuroxime solid dispersion with polyvinylpyrrolidone-10000, polyethylene glycol-400, and polyethylene glycol-1500 in a 1:2 ratio was studied for prolonged action compared to cefuroxime substance. The experimental formulations were studied for the parameters of gelation temperature in a long-term test (4 months), pH, and release of cefuroxime using dialysis bags. To study the distribution parameter in the vitreous body, an in vitro model (1/13) was developed, which was a hollow agar sphere filled with 1% (w/v) polyacrylate gel. For the superior formulations, a HET-CAM test (chorioallantoic membrane test) was performed to determine the absence of irritant effects. According to the study results, a formulation containing a solid dispersion of cefuroxime:PEG-400 (1:2), the matrix of which contained 18% (w/v) Kolliphor® P407 poloxamer, 3% (w/v) Kolliphor® P188 poloxamer, and 0.5% (w/v) hyaluronic acid (1400–1800), was selected. This sample had an average gelation temperature of 34.6 °C, pH 6.7 ± 0.5, and a pronounced prolonged effect. Only 7.6% was released in 3 h of the experiment, whereas about 38% of cefuroxime was released in 72 h. No irritant effect on the chorioallantoic membrane was observed for any formulations studied.

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Section: Methodsmentioning

confidence: 99%

Thermosensitive Intravitreal In Situ Implant of Cefuroxime Based on Poloxamer 407 and Hyaluronic Acid

Bakhrushina,

Dubova,

Nikonenko

et al. 2023

Gels

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“…Như vậy, kết quả phân tích nhiệt quét vi sai và phân tích nhiễu xạ tia X đã chứng minh rutin trong hệ phân tán rắn đã chuyển từ trạng thái kết tinh sang trạng thái vô định hình. Điều này cũng phù hợp với các nghiên cứu trước đây [9].…”

Section: Khảo Sát Một Số đặC Tính Hptr Rutin Bào Chế Theo Công Thức Tunclassified

Preparation of solid dispersion of rutin by spay drying

Khánh¹,

Thu²,

Tuấn³

2019

MPS

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The poor solubility of rutin leads to poor bioavailability. The present study is aimed to increase the solubility and bioavailability of rutin using solid dispersion technique. The solid dispersions of rutin were prepared by spray-dried method using β-CD, HPMC E6, HPMC E15, PVP K30, SLS, poloxamer 188 and Tween 80 as carriers. The interaction of rutin with the carriers was evaluated by using methods such as dissolved measurement, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The optimization of formulation was carried out by using Central Composite Face design. Independent variables include PVP K30/rutin ratio, Tween 80/rutin ratio, inlet air temperature, and feed flow rate. Dependent variables are the dissolution and product yield. The optimized preparation conditions for rutin solid dispersions were obtained as PVP K30: rutin at a ratio of 5.77, Tween 80: rutin at a ratio of 0.14, inlet temperature of 110.05, flow rate of 1370.9 ml per hour. The results of this study indicate that the solid dispersion of rutin increases significantly the dissolution of rutin in comparison with rutin. The results of the DSC and XRD studies prove the state transition of rutin from crystalline to amorphous. Keywords Rutin, solid dispersion, spray drying, PVP K30, dissolution. References [1] Beatriz Gullón, Thelmo A. Lú-Chau, María Teresa Moreira, Juan M. Lema, Gemman Eibes, Rutin: A review on extraction, identification and purification methods, biological activities and approaches to enhance its bioavailability, Trends in Food Science & Technology 67 (2017) 220-235. https://doi.org/10.1016/j.tifs.2017.07.008.[2] Carla Aparecida Pedriali, Adjaci Uchoa Fernandes, Leandra de Cássia Bernusso, Bronislaw Polakiewicz, The synthesis of a water-soluble derivative of rutin as an antiradical agent, Química Nova 31(8) (2008) 2147-2151. http://dx.doi.org/10.1590/S0100-40422008000800039.[3] Chiou, Win Loung, Riegelman, Sidney, Pharmaceutical applications of solid dispersion systems, Journal of pharmaceutical sciences 60(9) (1971) 1281-1302. https://doi.org/10.1002/jps.2600600902.[4] Xingwang Zhang, Huijie Xing,Yue Zhao, Zhiguo Ma, Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs, Pharmaceutics 10(3) (2018) 1-33. https://doi.org/10.3390/pharmaceutics10030074.[5] Ladan Akbarpour Nikghalb, Gurinder Singh, Gaurav Singh, Kimia Fazaeli Kahkeshan, Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs, Journal of Applied Pharmaceutical Science 2(10) (2012) 170-175. https://doi.org/10.7324/JAPS.2012.2103.[6] Amrit Paudel, Zelalem Ayenew Worku, Joke Meeus, Sandra Guns, Guy Van den Mooter, Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations, International Journal of Pharmaceutics 453(1) (2013) 253-284. https://doi.org/10.1016/j.ijpharm.2012.07.015.[7] P.B. Dalvi, A.B. Gerange, R. IngaleP, Solid dispersion: strategy to enhance solubility, Journal of Drug Delivery & Therapeutics 5(2) (2015) 20-28. https://doi.org/10.22270/jddt.v5i2.1060.[8] Chau Le Ngoc Vo, Chulhun Park, Beom Jin Lee, Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. European Journal of Pharmaceutics and Biopharmaceutics 85(3) (2013) 799-813. https://doi.org/10.1016/j.ejpb.2013.09.007.[9] I.V. Koval’skii, I.I. Krasnyuk, I.I. Krasnyuk, O.I. Nikulina, A.V. Belyatskaya, Yu. Ya. Kharitonov, N.B. Fel’dman, S.V. Lutsenko, V.V. Grikh, Studies of the Solubility of Rutin from Solid Dispersions, Pharmaceutical Chemistry Journal 47(11) (2014) 612-615. https://doi.org/10.1007/s11094-014-1020-z.

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“…Various systems have been developed and studied for rutin delivery including nanocrystals [13], nanostructured liquisolid systems [14], phytosomes [15], prenanoemulsion [16], solid lipid nanoparticles [17], metallic nanoparticles [18], polymeric nanoparticles [19], pH-sensitive nanospheres [20], and cyclodextrin inclusion complexes [21][22][23]. However, the incorporation of rutin into a solid dispersion with a hydrophilic polymer could be a simpler approach compared to the previously mentioned ones and was reported to be greatly successful in increasing rutin solubility and dissolution rate [24]. Moreover, the adaptation of colon targeted drug delivery approach is useful in directing drugs to cancer cells in colon, Advancements in Modified-release Oral Drug Delivery: Delivery Throughout the Gastro-intestinal tract which enhances therapeutic efficacy.…”

Section: Introductionmentioning

confidence: 99%

An Innovative Approach for Formulation of Rutin Tablets Targeted for Colon Cancer Treatment

2023

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The aim of this study was the improvement of rutin solubility along with targeting its release to colon for effective treatment of colon cancer. Five formulations of compression-coated tablets were prepared with the same core composition including rutin-polyvinyl pyrrolidone K30 solid dispersion (rutin-PVP K30 SD) but differ in being coated with either frankincense alone or different combinations of frankincense with gelatin. The superior formula was selected based on the in vitro drug release then further evaluated in terms of physical properties and in vivo performance in dogs using X-ray. Moreover, in vitro cytotoxicity of rutin, rutin-PVP K30 SD, frankincense, and a mixture of rutin-PVP K30 SD with frankincense in a ratio representing their concentrations in the selected formula was assessed against human colon cancer (HCT-116) cell lines using sulforhodamine B assay. The formula (F4) with the coat consisted of 65%w/w frankincense and 35%w/w gelatin achieved acceptable in vitro controlled drug release. In vivo X-ray in dogs confirmed that F4 tablet could remain intact in the stomach and small intestine until reaching the colon. In vitro cytotoxicity revealed that mixture of rutin-PVP K30 SD with frankincense was more effective in arresting cancer cell growth than rutin or frankincense alone. Moreover, stability studies revealed that F4 tablets were physically and chemically stable. Thus, improving rutin solubility using solid dispersion technique and formulating it into frankincense-based compression-coated (F4) tablets would be a successful approach for colonic delivery of rutin with potential of improving therapeutic efficacy. Graphical Abstract

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Studies of the Solubility of Rutin from Solid Dispersions

Cited by 8 publications

References 0 publications

Thermosensitive Intravitreal In Situ Implant of Cefuroxime Based on Poloxamer 407 and Hyaluronic Acid

Thermosensitive Intravitreal In Situ Implant of Cefuroxime Based on Poloxamer 407 and Hyaluronic Acid

Preparation of solid dispersion of rutin by spay drying

An Innovative Approach for Formulation of Rutin Tablets Targeted for Colon Cancer Treatment

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