Preparation and evaluation in vitro of salicylic acid-pachyman nanoparticles

Abstract

Pachyman based nanoparticles loading salicylic acid as model drug (SA-PNPs) were prepared by an inverse microemulsion crosslinking approach using epichlorohydrin (ECH) as crosslinker. The effects of crosslinking reaction time, initial volume ratio of oil to aqueous phase and dosage of crosslinker on the particle size of SA-PNPs were optimized by orthogonal experimental design. SA-PNPs prepared under the optimal conditions had the average size of 230 nm and high encapsulation efficiency of 90%. The in vitro drug release was also investigated and the release data were analyzed using zero order, first order and Higuchi’s kinetics model. According to the determined coefficients, release data fitted to Higuchi’s model, which suggested that the release of SA from SA-PNPs in phosphate buffer (pH 7.4) was diffusion controlled release. The experimental results indicated that pachyman possesses a promising potential to be applied as nanocarriers for controlled drug release.

Keywords

nanoparticles / pachyman / salicylic acid

References

[1] Kotwal V. B., Saifee M., Inamdar N., . Biodegradable Polymers: Which, When and Why? [J]. Indian J. Pharm. Sci., 2007, 69: 616-625.

[2] Oupicky D. Design and Development Strategies of Polymer Materials for Drug and Gene Delivery Applications [J]. Adv. Drug Deliver Rev., 2008, 60(9): 957

[3] Kvien I., Sugiyama J., Votrubec M., . Characterization of Starch Based Nnanocomposites [J]. J. Mater. Sci., 2007, 42(19): 8 163-8 171.

[4] Esposito E., Menegatti E., Cortesi R. Hyaluronan-based Microspheres as Tools for Drug Delivery: a Comparative Study [J]. Int. J. Pharm., 2005, 288(1): 35-49.

[5] Prabaharan M. Chitosan Derivatives as Promising Materials for Controlled Drug Delivery [J]. J. Biomater. Appl., 2008, 23(1): 5-36.

[6] Liu Z., Jiao Y., Wang Y., . Polysaccharides-based Nanoparticles as Drug Delivery Systems [J]. Adv. Drug Deliver Rev., 2008, 60(15): 1650-1662.

[7] Tønnesen H. H., Karlsen J. Alginate in Drug Delivery Systems [J]. Drug Dev. Ind. Pharm., 2002, 28(6): 621-630.

[8] Yin Y. J., Li Z. Y., Sun Y. B., . A preliminary study on Chitosan/gelatin Polyelectrolyte Complex Formation [J]. J. Mater. Sci., 2005, 40(17): 4649-4652.

[9] Rinaudo M. Main Properties and Current Applications of Some Polysaccharides as Biomaterials [J]. Polym. Int., 2008, 57: 397-430.

[10] Denkbas E. B. Perspectives on: Chitosan Drug Delivery Systems Based on Their Geometries [J]. J. Bioact. Compat. Pol., 2006, 21(4): 351-367.

[11] Yamada H., Kiyohara H., Takemoto N., . Studies on Immunologically Active Substances from Kampo Medicine, Juzen-taiho-to. 3. Mitogenic and Complement Activating Activities of the Herbal Components of Juzentaiho-to[J]. Planta Med., 1992, 58: 166-170.

[12] Wang Y. F., Zhang L. N., Li Y. Q., . Correlation of Structure to Antitumor Activities of Five Derivatives of a β-glucan from Poria Cocos Sclerotium[J]. Carbohydr. Res., 2004, 339: 2 567-2 574.

[13] Xiao Y. L., Liang S. C., Qiu G. F., . Preparation, Characterization and Tableting Properties of Two New Pachymanbased Pharmaceutical Aids: I. Disintegrants in Dispersible Tablets[J]. Polym. Adv. Tech., 2007, 18: 268-274.

[14] Xiao Y. L., Xu W. J., Zhu Q. F., . Preparation and Characterization of a Novel Pachyman-based Pharmaceutical Aid. II: A pH-sensitive, Biodegradable and Biocompatible Hydrogel for Controlled Release of Protein Drugs [J]. Carbohydr. Polym., 2009, 77: 612-620.

[15] Hu Y., Zhou X.J., Lu Y., . Novel Biodegradable Hydrogels Based on Pachyman and Its Derivatives for Drug Delivery[J]. Int. J. Pharm., 2009, 371: 89-98.

[16] Hu Y., He X. R., Lei L., . Preparation and Characterization of Self-assembled Nanoparticles of the Novelcarboxymethyl Pachyman-deoxycholic Acid Conjugates[J]. Carbohydr. Polym., 2008, 74: 220

[17] Mohanraj V. J., Chen Y. Nanoparticles[J]. Trop. J. Pharm. Res., 2006, 5(1): 561-573.

[18] Yih T. C., Al-Fandi M. Engineered Nanoparticles as Precise Drug Delivery Systems [J]. J. Cell Biochem., 2006, 97(6): 1 184-1 190.

[19] Eslamian M., Shekarriz M. Recent Advances in Nanoparticle Preparation by Spray and Micro-emulsion Methods[J]. Recent Pat. Nanotechnol., 2009, 3(2): 99-115.