Sirolimus solid self-microemulsifying pellets: Formulation development, characterization and bioavailability evaluation

Hu, Xiongwei; Chen, Lin; Chen, Dingxiong; Zhang, Jing; Liu, Zhihong; Wu, Wei; Hong-tao, Song

doi:10.1016/j.ijpharm.2012.07.055

Cited by 95 publications

(46 citation statements)

References 24 publications

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“…27 Similar yields were obtained from these three formulations, likely because the three proteins used have similar structures and physicochemical properties. [28][29][30] The surfaces of pellets layered with nanosuspensions stabilized by soybean protein isolate, whey protein isolate, or β-lactoglobulin were smooth ( Figure 3A1-C1) and each layer of solidified nanosuspension was tightly packed and could be distinguished easily from the pellet cores ( Figure 3A2-C2, 3A3-C3). …”

Section: Coating Nanosuspensions Onto Pelletsmentioning

confidence: 99%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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Background: Drug nanosuspensions are very promising for enhancing the dissolution and bioavailability of drugs that are poorly soluble in water. However, the poor stability of nanosuspensions, reflected in particle growth, aggregation/agglomeration, and change in crystallinity state greatly limits their applications. Solidification of nanosuspensions is an ideal strategy for addressing this problem. Hence, the present work aimed to convert drug nanosuspensions into pellets using fluid-bed coating technology. Methods: Indomethacin nanosuspensions were prepared by the precipitation-ultrasonication method using food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) as stabilizers. Dried nanosuspensions were prepared by coating the nanosuspensions onto pellets. The redispersibility, drug dissolution, solid-state forms, and morphology of the dried nanosuspensions were evaluated. Results: The mean particle size for the nanosuspensions stabilized using soybean protein isolate, whey protein isolate, and β-lactoglobulin was 588 nm, 320 nm, and 243 nm, respectively. The nanosuspensions could be successfully layered onto pellets with high coating efficiency. Both the dried nanosuspensions and nanosuspensions in their original amorphous state and not influenced by the fluid-bed coating drying process could be redispersed in water, maintaining their original particle size and size distribution. Both the dried nanosuspensions and the original drug nanosuspensions showed similar dissolution profiles, which were both much faster than that of the raw crystals. Conclusion: Fluid-bed coating technology has potential for use in the solidification of drug nanosuspensions.

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Section: Coating Nanosuspensions Onto Pelletsmentioning

confidence: 99%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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“…The solid-state is commonly characterized using differential scanning calorimetry (DSC) (Balakrishnan et al, 2009;Craig, 2006;Kang et al, 2012) or XRay powder diffraction (XRPD) (Docoslis et al, 2007;Hu et al, 2012;Wei et al, 2012) or vibrational spectroscopy (Milović et al, 2012;Nazzal et al, 2002;Stillhart and Kuentz, 2012). However these techniques are costly and require a highly trained user (for XRPD) and are destructive (for DSC).…”

Section: Introductionmentioning

confidence: 99%

Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Sacré

Netchacovitch

Bleye

et al. 2015

International Journal of Pharmaceutics

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Newly developed drugs often have poor bioavailability due to their poor water solubility (BCS class 2 drugs). It is therefore necessary to develop new strategies to enhance their solubility and their activity, among which, Self-Emulsifying Drug Delivery System (SEDDS).The efficacy of the drugs contained in these preparations is mainly affected by the solid state and the particle size of the active pharmaceutical ingredient (API).However, it is quite complex, long and expensive to characterize these parameters with classical techniques such as X-Ray powder diffraction, differential scanning calorimetry or hot stage microscopy.The present article presents, through a case study, the advantages of the Raman hyperspectral imaging in the characterization of such formulations. Indeed, Raman chemical imaging may fully characterize SEDDS with single equipment and operator in a non-destructive way allowing the follow-up of the formulation during stability studies. Raman imaging is therefore a tool of choice in the PAT framework since it increases the knowledge of the formulation and the process. 2A quantitative multivariate method using Raman hyperspectral imaging to assay the API in the lipid based formulation has been developed and fully validated following the "total error" approach.

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“…Then, the particle size decreased with the increasingly emulsifying ability. The emulsification time increased with the increase of the ratio of oil phase or K m (The relative decrease of emulsifying ability is the fact that the percent of surfactant is lower compared with oil) (13).…”

Section: Properties Of Puerarin Liquid Self-microemulsionmentioning

confidence: 99%

“…Therefore, a new preparation of administration is necessary to overcome these problems. Methods of improving drug solubility including solid dispersion, nanoemulsions, polymer micelles, liposomes, cyclodextrin (CD) inclusion, and self-emulsifying drug delivery system are adopted to develop the oral drug delivery system (9)(10)(11)(12)(13)(14). Self-microemulsifying drug delivery system (SMEDDS), a valid pharmaceutical technology to increase solubility and absorption of poorly water-soluble drugs in vivo, has recently received increasing attention as a kind of new drug delivery systems.…”

mentioning

confidence: 99%

Preparation and In Vitro/In Vivo Evaluation of Puerarin Solid Self-Microemulsifying Drug Delivery System by Spherical Crystallization Technique

Cheng

et al. 2015

AAPS PharmSciTech

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Abstract. The aim of this work was to establish a method for preparing stable and controllable solid selfmicroemulsifying drug delivery system (S-SMEDDS) by spherical crystallization technique, which was explored for promoting the dissolution, oral bioavailability, and process efficiency. Solubility test, preparation of liquid self-microemulsifying drug delivery system (L-SMEDDS), and the obtained ternary phase diagrams test have been performed to screen and optimize the composition of LSMEDDS. The optimized formulation was used to prepare puerarin solid self-microemulsifying drug delivery system (Pue-SSMEDDS) by spherical crystallization technique. Droplet size and morphological analysis of the optimal Pue-SSMEDDS were determined to evaluate the final formulation. And the Pue-SSMEDDS was also assessed by flowability study, angle of repose, Carr's index, and flow velocity. Furthermore, the vitro dissolution and pharmacokinetic profile in vivo were analyzed. The study in vitro showed the Pue-SSMEDDS could disperse in the dispersion medium within 60 s and was spherical with the particle size of 19.66 nm and zeta potential of −28.3 mV. It could keep stable at low temperature and seal condition for 3 months. In vivo pharmacokinetic experiments of rats, the mean plasma concentration of selfmicroemulsion group was much higher than that of conventional tablets and could play a long-lasting efficacy, while there was no significant difference between the LSMEDDS and S-SMEDDS. The results suggested the potential of S-SMEDDS could improve the oral bioavailability of poorly water-soluble drug, such as puerarin.

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Sirolimus solid self-microemulsifying pellets: Formulation development, characterization and bioavailability evaluation

Cited by 95 publications

References 24 publications

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Thorough characterization of a Self-Emulsifying Drug Delivery System with Raman hyperspectral imaging: A case study

Preparation and In Vitro/In Vivo Evaluation of Puerarin Solid Self-Microemulsifying Drug Delivery System by Spherical Crystallization Technique

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