Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility

Abstract

Background: The objective of this study was to evaluate fluid-bed coating as a new technique to prepare a pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporin A as a model of a poorly water-soluble drug. Methods: The rationale of this technique was to entrap a Liquid SNEDDS in the matrix of the coating material, polyvinylpyrrolidone K30, by fluid-bed coating. Pseudoternary phase diagrams were used to screen the liquid SNEDDS formulations. The optimal formulation was composed of Labrafil M ® 1944 CS, Transcutol P ® , and Cremophor ® EL in a ratio of 9:14:7. To prepare solid SNEDDS pellets, liquid SNEDDS was first dispersed in an aqueous solution of polyvinylpyrrolidone and then sprayed onto the surface of non-pareil pellets. Upon evaporation of water, polyvinylpyrrolidone precipitated and formed tight films to entrap the liquid SNEDDS. Visual observation and scanning electron microscopic analysis confirmed good appearance of the solid SNEDDS pellets. Results: Our results indicated that up to 40% of the liquid SNEDDS could be entrapped in the coating layer. Powder x-ray diffraction analysis confirmed nonexistence of crystalline cyclosporin A in the formulation. Solid SNEDDS pellets showed a slower redispersion rate than the liquid SNEDDS. An increase in the total liquid SNEDDS loading led to faster redispersion, whereas increased coating weight (up to 400%) significantly decreased the redispersion rate. Both cyclosporin A loading and protective coating with 5% polyvinylpyrrolidone K30 did not significantly affect the redispersion rate. Conclusion: It is concluded that fluid-bed coating is a new technique with considerable potential for preparation of pellet-based solid SNEDDS formulations.

Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility

“…Samples were gold-coated by Q150R sputter coater (Quorum Technologies Ltd, East Sussex, UK). The process was carried out in an argon atmosphere, at 20 mA for 1 min and involved applying 3–10 KV excitation electron energy [ 30 ]. Sieve analysis study was performed for pellet size distribution.…”

Design and Characterization of Cyclosporine A-Loaded Nanofibers for Enhanced Drug Dissolution

“…Diffraction patterns of pure TPGS, F127, and CyA were used as references for the evaluation of various micellar nanoformulations. Reference spectra indicated that CyA existed in a crystalline state before incorporation into the micellar formulations (Figure ia); the diffractogram of raw CyA powder showed characteristic high-intensity diffraction peaks at 2θ values of 6.86° (011), 7.8° (102), 9.26° (110), 10.76° (112), 12.58° (022), 14.48° (201), 15.04° (202), 15.2° (210), 16.78° (124), 18.6° (131), 19.38° (132), 20.84° (027), 22.14° (230), 23.28° (042), and 24.28° (119). , Pure F127 also showed two characteristic peaks with the highest intensity at 2θ angles 19.13 and 23.32°, indicating that F127 is a crystalline adjuvant . The characteristic peaks 18.12 and 22.32° of TPGS were observed in the diffraction pattern of TPGS .…”

“…042), and 24.28°(119). 30,31 Pure F127 also showed two characteristic peaks with the highest intensity at 2θ angles 19.13 and 23.32°, indicating that F127 is a crystalline adjuvant. 32 The characteristic peaks 18.12 and 22.32°of TPGS were observed in the diffraction pattern of TPGS.…”

How to Improve Solubility and Dissolution of Irbesartan by Fabricating Ternary Solid Dispersions: Optimization and In-Vitro Characterization

“…Kolliphor ® P 407 showed two peaks at 19.346 • and 23.472 • angles (2 θ) [16]. Polyvinylpyrrolidone-K30 did not show these typical diffraction peaks due to its amorphous nature [39], indicating a broad and diffused pattern as its molecules are randomly arranged in a crystal lattice [40]. Furthermore, the PXRD of formulation KP407 (TD 3 ) with 1:4:3 ratio (drug: binary polymer:ternary polymer) revealed only one small peak, reflecting a high conversion of crystalline drug into amorphous form.…”