Thermolysin catalyses the synthesis of cyclodextrin esters in DMSO

Pedersen, Ninfa Rangel; Kristensen, Janni Brogaard; Bauw, Guy; Ravoo, Bart Jan; Darcy, Raphael; Larsen, Kim Lambertsen; Pedersen, Lars Haastrup

doi:10.1016/j.tetasy.2004.12.009

Cited by 47 publications

(29 citation statements)

References 26 publications

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“…During this stage, swelling of the carbopol occurs due to absorption of water from mucus layer which causes intimate penetration into the mucus and hence localizes the formulation in nasal cavity, enhancing the drug concentration gradient across the epithelium. This results in rapid dissolution and diffusion of drug from the gels due to extensive swelling of the ionized carbopol (17). Based on this explanation highest drug permeation of 97.74% in 6 h was demonstrated by F8 (LOR complex, 1% w/v carbopol and 20% w/v poloxamer) and least permeation of 64.81% was shown by F5 within 6 h (LOR, 0.5% w/v carbopol and 20% w/v poloxamer).…”

Section: Ex Vivo Permeationmentioning

confidence: 96%

Thermally Triggered Mucoadhesive In Situ Gel of Loratadine: β-Cyclodextrin Complex for Nasal Delivery

2013

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Abstract. The aim of the present study was to increase the solubility of an anti-allergic drug loratadine by making its inclusion complex with β-cyclodextrin and to develop it's thermally triggered mucoadhesive in situ nasal gel so as to overcome first-pass effect and consequently enhance its bioavailability. A total of eight formulations were prepared by cold method and optimized by 2 3 full factorial design. Independent variables (concentration of poloxamer 407, concentration of carbopol 934 P, and pure drug or its inclusion complex) were optimized in order to achieve desired gelling temperature with sufficient mucoadhesive strength and maximum permeation across experimental nasal membrane. The design was validated by extra design checkpoint formulation (F9) and Pareto charts were used to help eliminate terms that did not have a statistically significant effect. The response surface plots and possible interactions between independent variables were analyzed using Design Expert Software 8.0.2 (Stat Ease, Inc., USA). Faster drug permeation with zero-order kinetics and target flux was achieved with formulation containing drug: β-cyclodextrin complex rather than those made with free drug. The optimized formulation (F8) with a gelling temperature of 28.6±0.47°C and highest mucoadhesive strength of 7,676.0±0.97 dyn/cm 2 displayed 97.74±0.87% cumulative drug permeation at 6 h. It was stable for over 3 months and histological examination revealed no remarkable damage to the nasal tissue.

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Section: Ex Vivo Permeationmentioning

confidence: 96%

Thermally Triggered Mucoadhesive In Situ Gel of Loratadine: β-Cyclodextrin Complex for Nasal Delivery

2013

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“…1 and 2. Several characteristic IR absorption bands for LOR, β-CD or HP-β-CD may be assigned as follows: 1703 cm -1 (C=O of ester), 1560, 1474 and 1434 cm -1 (stretching vibrations of benzene ring), 1227 cm-1 (C-O stretching) for LOR; 1644 or 1646 cm −1 (OH groups of the glucose moieties) for β-CD or HP-β-CD, respectively (Nacsa et al, 2008(Nacsa et al, , 2009Zhao et al, 2003;Pedersen et al, 2005). In the LOR/β-CD mixture, four new peaks at 1675, 1478, 1440 and 1236 cm -1 were clearly observed after grinding for 15 min.…”

Section: Grinding-induced Ftir Spectral Shifts Of Lor In the Presencementioning

confidence: 99%

Thermodynamic Study of Grinding-Induced Loratadine Inclusion Complex Formation Using Thermal Analysis and Curve-Fitted FTIR Determination

Lin¹,

Lin²,

Lin³

et al. 2011

Thermodynamics - Physical Chemistry of Aqueous Systems

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“…β -Cyclodextrin and its methyl and hydroxypropyl derivatives were acylated by means of lipases with a series of carboxylic acids [81] , and the synthesis of CD fatty acid esters was enzymatically catalyzed by some proteases [82] . β -Cyclodextrin and its methyl and hydroxypropyl derivatives were acylated by means of lipases with a series of carboxylic acids [81] , and the synthesis of CD fatty acid esters was enzymatically catalyzed by some proteases [82] .…”

Section: Enzymatic Synthesis Of Cyclodextrin -Derivativesmentioning

confidence: 99%