Development and pharmacological evaluation of ropivacaine-2-hydroxypropyl-β-cyclodextrin inclusion complex

Araújo, Daniele Ribeiro de; Tsuneda, Simone Sayuri; Cereda, Cíntia Maria Saia; Carvalho, Fernanda Del Grossi Ferraz; Prete, Paulo Sergio Castilho; Fernandes, Sérgio Antônio; Yokaichiya, Fabiano; Franco, Margareth K. K. D.; Mazzaro, I.; Fraceto, Leonardo Fernandes; Braga, Angélica de Fátima de Assunção; Paula, Eneida de

doi:10.1016/j.ejps.2007.09.010

Cited by 133 publications

(93 citation statements)

References 39 publications

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“…SEM is a qualitative method used to investigate the surface morphology of drugs, CDs, and other materials (35,36). Figure S1 displays the SEM images of all the samples.…”

Section: Semmentioning

confidence: 99%

Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin

Tang

Wang²,

et al. 2016

AAPS PharmSciTech

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Abstract. Posaconazole is a triazole antifungal drug that with extremely poor aqueous solubility. Up to now, this drug can be administered via intravenous injection and oral suspension. However, its oral bioavailability is greatly limited by the dissolution rate of the drug. This study aimed to improve water solubility and dissolution of posaconazole through characterizing the inclusion complexes of posaconazole with β-cyclodextrin (β-CD) and 2,6-di-O-methyl-β-cyclodextrin (DM-β-CD). Phase solubility studies were performed to calculate the stability constants in solution. The results of FT-IR, PXRD, 1 H and ROESY 2D NMR, and DSC all verified the formation of the complexes in solid state. The complexes showed remarkably improved water solubility and dissolution rate than pure posaconazole. Especially, the aqueous solubility of the DM-β-CD complex is nine times higher than that of the β-CD complex. Preliminary in vitro antifungal susceptibility tests showed that the two inclusion complexes maintained high antifungal activities. These results indicated that the DM-β-CD complexes have great potential for application in the delivery of poorly water-soluble antifungal agents, such as posaconazole.

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“…SEM is a qualitative method used to investigate the surface morphology of drugs, CDs, and other materials (35,36). Figure S1 displays the SEM images of all the samples.…”

Section: Semmentioning

confidence: 99%

Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin

Tang

Wang²,

et al. 2016

AAPS PharmSciTech

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“…We intend to mask the bitter taste of injectable LID using 2-hydroxypropylbeta-cyclodextrin (HP-β-CD) and sodium saccharin. HP-β-CD is an alkylated derivative of β-cyclodextrin with greater aqueous solubility, improved complexing ability, and less toxicity (15)(16)(17). Hence, HP-β-CD has been used as an excipient in various injectable formulations in order to increase aqueous solubility of drugs.…”

Section: Introductionmentioning

confidence: 99%

Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

et al. 2014

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Abstract. Several attempts have been made to mask the bitter taste of oral formulations, but none have been made for injectable formulations. This study aims to mask the bitter taste of dental lidocaine HCl (LID) injection using hydroxypropyl-β-cyclodextrin (HP-β-CD) and sodium saccharin. Inclusion complexes of LID and HP-β-CD were prepared by the solution method in 1:1 and 1:2 M ratios. Inclusion complexes in solution were studied using phase solubility in phosphate buffer solutions (pH 8, 9, and 10). Freeze-dried inclusion complexes were characterized using differential scanning calorimetry (DSC), Xray, Fourier transform infrared (FT-IR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), and in vitro release. Injectable formulations were prepared using inclusion complexes and characterized for stability and for taste using an Alpha MOS ASTREE electronic tongue (ETongue). The association constants of HP-β-CD with lidocaine-free base and its ionized form were found to be 26.23± 0.00025 and 0.8694±0.00045 M −1 , respectively. Characterization studies confirmed the formation of stable inclusion complexes of LID and HP-β-CD. Injectable formulations were found to be stable for up to 6 months at 4°C, 25°C, and 40°C. The taste evaluation study indicated that HP-β-CD (1:1 and 1:2 M ratios) significantly improved the bitter taste of LID injectable formulation. In conclusion, inclusion complex in the 1:1 M ratio with 0.09% sodium saccharin was considered to be optimum in masking the bitter taste of LID.

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“…They are able to form inclusion complexes with lipophilic guest molecules which have been shown to improve aqueous solubility, dissolution rate, and bioavailability of such drugs (19,20). Due to the solubility, hygroscopicity, and toxicity concerns of CDs, they were modified to randomly methylated β-CD (RM β-CDs).…”

Section: Introductionmentioning

confidence: 99%

Novel Vitamin and Gold-Loaded Nanofiber Facial Mask for Topical Delivery

et al. 2010

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Abstract. L-ascorbic acid has been widely used in cosmetic and dermatological products because of its ability to scavenge free radicals and destroy oxidizing agents. However, it is chemically unstable and can easily be oxidized. The current cosmetic facial masks available in the market are pre-moistened, which means that the aqueous fluid content of the mask may oxidize some of the unstable active ingredients such as ascorbic acid. This work presents an anti-wrinkle nanofiber face mask containing ascorbic acid, retinoic acid, gold nanoparticles, and collagen. This novel face mask will only be wetted when applied to the skin, thus enhancing product stability. Once moistened, the content of the mask will gradually dissolve and release the active ingredients and ensure maximum skin penetration. The high surface areato-volume ratio of the nanofiber mask will ensure maximum contact with the skin surface and help to enhance the skin permeation to restore its healthy appearance. Electrospun fiber mats may provide an attractive alternative to the commercial facial cotton masks.

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Development and pharmacological evaluation of ropivacaine-2-hydroxypropyl-β-cyclodextrin inclusion complex

Cited by 133 publications

References 39 publications

Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin

Characterization and In Vitro Evaluation of the Complexes of Posaconazole with β- and 2,6-di-O-methyl-β-cyclodextrin

Masking the Bitter Taste of Injectable Lidocaine HCl Formulation for Dental Procedures

Novel Vitamin and Gold-Loaded Nanofiber Facial Mask for Topical Delivery

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