A lipid-based liquid crystalline matrix that provides sustained release and enhanced oral bioavailability for a model poorly water soluble drug in rats

Boyd, Ben J.; Khoo, Shui Mei; Whittaker, Darryl V.; Davey, Greg; Porter, Christopher John

doi:10.1016/j.ijpharm.2007.03.020

Cited by 161 publications

(103 citation statements)

References 25 publications

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“…16 Most studies have focused on glyceryl monooleate (GMO) as a liquid crystal-forming lipid, but glyceride lipids possess ester bonds that are susceptible to degradation by lipase enzymes in the GIT. This phenomenon was previously observed with GMO cubosomes in in vitro digestion models, 17 implying a loss of liquid crystal structure in vivo. Therefore, non-digestible lipid phytantriol (PYT) has attracted increasing interest due to its similar phase behavior as GMO's and improved chemical stability.…”

Section: Introductionsupporting

confidence: 72%

“…Similar results were also reported in previous literature. 17,23 In the current study, the initial burst release of ibuprofen from cubic nanoparticles was probably attributed to either the surface-bound moieties or an aqueous environment allowing increased water penetration. Afterwards, the cubic nanoparticles manifested the sustained release characteristics that appeared to be dependent on the hydrophobicity of ibuprofen incorporated in the cubic nanoparticles.…”

Section: Discussionmentioning

confidence: 63%

“…After administration, about 3 mL of blood was collected from the hind leg vein into heparinized tubes at time intervals of 0. 17 …”

Section: In Vivo Pharmacokinetics Studymentioning

confidence: 99%

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Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Dian¹,

Yang²,

Li³

et al. 2013

IJN

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Abstract:In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P , 0.05). The ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment.

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Section: Introductionsupporting

confidence: 72%

Section: Discussionmentioning

confidence: 63%

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Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Dian¹,

Yang²,

Li³

et al. 2013

IJN

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“…These results were consistent with those of a previous study in which the T max after administration in the upper small intestine was delayed by cubosome carriers. 34,35 Meanwhile the clearance of PPD-cubosome and raw PPD had no significant change. Additionally, the clearance of PPD-cubosome loaded with piperine was lower than that of PPD-cubosome because of the inhibition of metabolism of PPD induced by piperine.…”

Section: Pharmacokinetics Of Ppd and Ppdcubosome After Oral Administrmentioning

confidence: 96%

Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies

Jin¹,

Zhang²,

Sun³

et al. 2013

IJN

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Background: 20(S)-protopanaxadiol (PPD), similar to several other anticancer agents, has low oral absorption and is extensively metabolized. These factors limit the use of PPD for treatment of human diseases. Methods: In this study, we used cubic nanoparticles containing piperine to improve the oral bioavailability of PPD and to enhance its absorption and inhibit its metabolism. Cubic nanoparticles loaded with PPD and piperine were prepared by fragmentation of glyceryl monoolein (GMO)/poloxamer 407 bulk cubic gel and verified using transmission electron microscopy and differential scanning calorimetry. We evaluated the in vitro release of PPD from these nanoparticles and its absorption across the Caco-2 cell monolayer model, and subsequently, we examined the bioavailability and metabolism of PPD and its nanoparticles in vivo. Results: The in vitro release of PPD from these nanoparticles was less than 5% at 12 hours. PPDcubosome and PPD-cubosome loaded with piperine (molar ratio PPD/piperine, 1:3) increased the apical to basolateral permeability values of PPD across the Caco-2 cell monolayer from 53% to 64%, respectively. In addition, the results of a pharmacokinetic study in rats showed that the relative bioavailabilities of PPD-cubosome [area under concentration-time curve (AUC) 0-∞ ] and PPD-cubosome containing piperine (AUC 0-∞ ) compared to that of raw PPD (AUC 0-∞ ) were 166% and 248%, respectively. Conclusion: The increased bioavailability of PPD-cubosome loaded with piperine is due to an increase in absorption and inhibition of metabolism of PPD by cubic nanoparticles containing piperine rather than because of improved release of PPD. The cubic nanoparticles containing piperine may be a promising oral carrier for anticancer drugs with poor oral absorption and that undergo extensive metabolism by cytochrome P450.

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“…Whereas 5 % IMC-CCC-LA release rate constant was 97.3 μg mL −1 h −1/2 . CCC may work as a matrix in the mixture (34). As the concentrations of IMC increased from 1 to 5 %, the release rate constants in CCC were significantly increased (p<0.05).…”

Section: Dissolution Test Of Imc-ccc Imc-ccc-la Mixturementioning

confidence: 97%

Physicochemical Performances of Indomethacin in Cholesteryl Cetyl Carbonate Liquid Crystal as a Transdermal Dosage

et al. 2012

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Abstract. A transdermal formulation of indomethacin (IMC) was developed by incorporation into cholesteryl cetyl carbonate (CCC). The liquid crystalline phase properties of the IMC-CCC mixture were detected by polarized light microscopy and differential scanning calorimetry. A low drug loading was obtained (1-5 %) similar to that used in conventional topical IMC in a clinical setting. A controlled release of IMC was found over 12 h. A low amount of IMC in 1 % IMC-CCC permeated the stratum corneum. Further formulation development has been carried out by the addition of lauryl alcohol into 5 % IMC-CCC mixture it was found that the permeation of IMC was significantly improved to 45 % within 24 h.

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A lipid-based liquid crystalline matrix that provides sustained release and enhanced oral bioavailability for a model poorly water soluble drug in rats

Cited by 161 publications

References 25 publications

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Cubic phase nanoparticles for sustained release of ibuprofen formulation characterization and enhanced bioavailability study

Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies

Physicochemical Performances of Indomethacin in Cholesteryl Cetyl Carbonate Liquid Crystal as a Transdermal Dosage

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