Laponite-based nanohybrid for enhanced solubility and controlled release of itraconazole

Jung, Hyun Suk; Kim, Hyun Mi; Choy, Young Bin; Hwang, Seong Ju; Choy, Jin Ho

doi:10.1016/j.ijpharm.2007.08.008

Cited by 100 publications

(63 citation statements)

References 29 publications

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“…No XRD peaks of intact crystalline APZ were observed after hybridization, thus suggesting that the APZ molecules were distributed within the MMT interlayer space on a molecular level, as previously reported for other nanohybrid systems. [19][20][21] Considering the layer thickness of MMT (9.3 ), the gallery height of APZ-MMT could be estimated to be 11.7 (21.0À9.3 = 11.7 ).…”

Section: Resultsmentioning

confidence: 99%

AripiprazoleMontmorillonite: A New Organic–Inorganic Nanohybrid Material for Biomedical Applications

Choi

Choy

et al. 2013

Chemistry A European J

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Poor aqueous solubility and the unpleasant taste of aripiprazole (APZ) have been recurring problems, owing to its low bioavailability and low patient tolerance, respectively. Herein, we prepared a nanohybrid system that was based on a bentonite clay material, montmorillonite (MMT), which could both mask the taste and enhance the solubility of APZ (i.e., APZ-MMT). To further improve the efficacy of this taste masking and drug solubility, APZ-MMT was also coated with a cationic polymer, polyvinylacetal diethylamino acetate (AEA). In vitro dissolution tests at neutral pH showed that the amount of drug that was released from the AEA-coated APZ-MMT was greatly suppressed (<1%) for the first 3 min, thus suggesting that AEA-coated APZ-MMT has strong potential for the taste masking of APZ. Notably, in simulated gastric juice at pH 1.2, the total percentage of APZ that was released within the first 2 h increased up to 95% for AEA-coated APZ-MMT. Furthermore, this in vitro release profile was also similar to that of Abilify®, a commercially available medication. In vivo experiments by using Sprague-Dawley rats were also performed to compare the pharmacokinetics of AEA-coated APZ-MMT and Abilify®. AEA-coated APZ-MMT exhibited about 20% higher systemic exposure of APZ and its metabolite, dehydro-APZ, compared with Abilify®. Therefore, a new MMT-based nanovehicle, which is coated with a cationic polymer, can act as a promising delivery system for both taste masking and for enhancing the bioavailability of APZ.

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Section: Resultsmentioning

confidence: 99%

AripiprazoleMontmorillonite: A New Organic–Inorganic Nanohybrid Material for Biomedical Applications

Choi

Choy

et al. 2013

Chemistry A European J

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“…Their swelling transition [10], on the other hand, suggests their potential as hosts of large molecules of pharmaceutical interest and their temperature controlled release. However, few reports about the use of fluorohectorite, a commercially available synthetic smectite, as a drug hosting material, can be found in the literature [5,6,11]. From the structural point of view, in their dry form, the layers assemble to form stack-of-card like particles.…”

Section: Introductionmentioning

confidence: 99%

Smectite as ciprofloxacin delivery system: Intercalation and temperature-controlled release properties

Rivera

Valdés

Jiménez

et al. 2016

Applied Clay Science

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Ciprofloxacin (Cipro) incorporation into Li-fluorhectorite (LiFh) clay and its temperaturecontrolled release. with potential pharmaceutical and biomedical applications.Structural characterization of the raw material and the clay-drug composites.Demonstration of the temperature-controlled drug release abilities of a colloidal suspension of the clay-drug composite, following pharmaceutical standards. AbstractClays have shown to be good candidates as drug delivery carriers. In the present paper, we use the temperature-dependent swelling of smectite clays to produce clay-drug composites with sizable drug load capacity. Specifically, we obtain a fluorohectorite-ciprofloxacin (Fh-Cipro) composite, in which a true intercalation of the drug between the clay interlayers has been verified by various experimental techniques. We evaluate the thermally activated drug release from a colloidal suspension of nanosized composite particles in water as well as in synthetic gastric juice from 37 0 C (body temperature) to 85 0 C. The temporal profiles of drug release from the clay fulfil the pharmaceutical standards for these systems. In this work, we have been able to produce a clay-based Temperature Controlled Release System (TCRS) with potential biomedical applications.

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“…Thus, since A c is larger than 2A e , SDN molecules should have a tilted bilayer arrangement to avoid steric hindrance. 31,42 The protonation sites of SDN should be only at N22 as shown in Figure 1 since protonation in combined rings of pyrimidine and pyrazole is unlikely due to resonance and steric effects. 43 As a result, the SDN molecules should be arranged in the interlayer space of MMT as depicted in Figure 3A.…”

Section: Resultsmentioning

confidence: 99%

“…The cationic macromolecule, AEA, when dissolved and ionized selectively at low pH, could replace the intercalated drug molecules effectively and enlarge the interlayer spacing to facilitate drug diffusion out towards the release media. 31 This result is meaningful in a sense that AEA-coated SDN-MMT nanohybrids could provide both taste masking and effective in vitro release of SDN relatively similar to proven medications like Viagra ® .…”

Section: In Vitro Drug Release Testmentioning

confidence: 87%

“…For the latter, we reported that the presence of a large molecule possessing the same polarity as the intercalated compound facilitated the diffusion of the intercalated compound by enlarging the entrance of layered structures of MMT. [30][31][32] The carrier material, MMT clay, employed in this work is approved by the US Food and Drug Administration (FDA) as a diluting agent for oral delivery and is widely used in medicine and pharmacology. 33,34 The polymer used for coating, AEA, is also accepted as a food additive by the FDA.…”

Section: Introductionmentioning

confidence: 99%

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A nanohybrid system for taste masking of sildenafil

Lee¹,

Choi²,

Oh³

et al. 2012

IJN

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A nanohybrid was prepared with an inorganic clay material, montmorillonite (MMT), for taste masking of sildenafil (SDN). To further improve the taste-masking efficiency and enhance the drug-release rate, we coated the nanohybrid of SDN-MMT with a basic polymer, polyvinylacetal diethylaminoacetate (AEA). Powder X-ray diffraction and Fourier transform infrared experiments showed that SDN was successfully intercalated into the interlayer space of MMT. The AEA-coated SDN-MMT nanohybrid showed drug release was much suppressed at neutral pH (release rate, 4.70 ± 0.53%), suggesting a potential for drug taste masking at the buccal cavity. We also performed in vitro drug release experiments in a simulated gastric fluid (pH = 1.2) and compared the drug-release profiles of AEA-coated SDN-MMT and Viagra ® , an approved dosage form of SDN. As a result, about 90% of SDN was released from the AEAcoated SDN-MMT during the first 2 hours while almost 100% of drug was released from Viagra ® . However, an in vivo experiment showed that the AEA-coated SDN-MMT exhibited higher drug exposure than Viagra ® . For the AEA-coated SDN-MMT, the area under the plasma concentration-time curve from 0 hours to infinity (AUC 0-∞ ) and maximum concentration (C max ) were 78.8 ± 2.32 µg ⋅ hour/mL and 12.4 ± 0.673 µg/mL, respectively, both of which were larger than those obtained with Viagra ® (AUC 0-∞ = 69.2 ± 3.19 µg ⋅ hour/mL; C max = 10.5 ± 0.641 µg/mL).Therefore, we concluded that the MMT-based nanohybrid is a promising delivery system for taste masking of SDN with possibly improved drug exposure.

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Laponite-based nanohybrid for enhanced solubility and controlled release of itraconazole

Cited by 100 publications

References 29 publications

AripiprazoleMontmorillonite: A New Organic–Inorganic Nanohybrid Material for Biomedical Applications

AripiprazoleMontmorillonite: A New Organic–Inorganic Nanohybrid Material for Biomedical Applications

Smectite as ciprofloxacin delivery system: Intercalation and temperature-controlled release properties

A nanohybrid system for taste masking of sildenafil

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