Development and Characterization of Aspirin-Phospholipid Complex for Improved Drug Delivery

DOI:

https://doi.org/10.37285/ijpsn.2010.3.2.7

Authors

  • A Semalty
  • M Semalty
  • D Singh
  • M S M Rawat

Abstract

Aspirin (acetylsalicylic acid) is one of the most widely used analgesic.  Aspirin is poorly soluble in water and causes gastrointestinal (GI) irritation. To improve the solubility (and hence the bioavailability) and minimize the GI irritation, its complexes with soya-phospholipid-80 % (in  1: 1 molar ratio) were prepared in an organic solvent and evaluated for solubility, drug content, scanning electron microscopy (SEM), FT-IR spectra, X ray diffraction, differential scanning calorimetry (DSC) and in vitro dissolution study. Aspirin-phospholipid complex were found to be disc shaped with rough surface in SEM. Drug content in the complex was found to be 95.6 %. DSC thermograms, XRD and FTIR confirmed the formation of phospholipid complex. Solubility of the prepared complex was found to be improved. Aspirin complex and aspirin showed 90.93 % and 69.42 % of drug release at the end of 10 h in dissolution study in pH 1.2 acid buffer. It was concluded that the phospholipid complex of aspirin may be of potential use for improving the solubility of aspirin and hence its bioavailability. The complexes may also reduce GI toxicity of the drug.  

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Pharmacosomes, Phospholipids complex, Aspirin, NSAIDs

Downloads

Published

2010-08-31

How to Cite

1.
Semalty A, Semalty M, Singh D, Rawat MSM. Development and Characterization of Aspirin-Phospholipid Complex for Improved Drug Delivery. Scopus Indexed [Internet]. 2010 Aug. 31 [cited 2024 Apr. 19];3(2):940-7. Available from: https://www.ijpsnonline.com/index.php/ijpsn/article/view/498

Issue

Section

Research Articles

References

Biju SS, Talegaonkar S, Mishra PR, Khar RK. Vesicular Systems: An Overview. Indian J. Pharm. Sci. 68: 141-153 (2006).

Cui F, Shi K, Zhang L, Tao A, Kawashima Y. Biodegradable nanoparticles loaded with insulin-phospholipid complex for oral delivery : Preparation, in vitro characterization and in vivo evaluation. J. Control. Release. 114: 242-250 (2006).

Hollander MD. Gastrointestinal complications of non steroidal anti-inflammatory drugs: prophylactic and therapeutic strategies. Am. J. Med. 96: 274-81 (1994).

Jarmer DJ, Lengsfeld CS, Anseth KS, Randolph TW. Supercritical fluid crystallization of griseofulvin: Crystal habit modification with a selective growth inhibitor. J. Pharm. Sci. 94: 2688-2702 (2005).

Kesisoglon F, Panmai S, Wu Y. Nanosizing oral formulation development and biopharmaceutical evaluation. Adv. Drug. Dev. Rev. 59: 631–644 (2007).

Leuner C, Dressmann J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. BioPharm. 54: 107–112 (2002).

Li Y, Yang DJ, Chen SL, Chen SB, Chan ASC. Comparative physicochemical characterization of phospholipids complex of puerarin formulated by conventional and supercritical methods. Pharm. Res. 25: 563-77 (2007).

Lichtenberger LM, Wang ZM, Romero JJ, Ulloa C, Perez JC, Giraud MN, Barreto JC. Non steroidal anti-inflammatory drugs (NSAIDs) associate with zwitterionic phospholipids: Insight into the mechanism and reversal of NSAID-induced gastrointestinal injury. Nature Med. 11: 154-158 (1995).

Lúcio M, Bringezu F, Reis S, Lima JL, Brezesinski G. Binding of nonsteroidal anti-inflammatory drugs to DPPC: structure and thermodynamic aspects. Langmuir 15: 4132-9 (2008).

Maiti K, Mukherjee K, Gantait A, Saha BP, Mukherjee PK. Curcumin-phospholipid complex: Preparation, therapeutic evaluation and pharmacokinetic study in rats. Int. J. Pharm. 330: 155-163 (2007).

Nijlen TV, Brennan K, Mooter VG, Blaton N, Kinget R, Augustijns P. Improvement of the dissolution rate of artemisinin by means of supercritical fluid technology and solid dispersions. Int. J. Pharm. 254: 173–181 (2003).

Nokhodchi A. The effect of type and concentration of vehicles on the dissolution rate of a poorly soluble drug (indomethacin) from liquisolid compacts. J Pharm. Pharmaceutical Sci. 8: 18-25 (2005).

Patravale VB, Date AA, Kulkarni RM. Nanosuspensions: a promising drug delivery strategy. J. Pharm. Pharmacol. 56: 827–840 (2004).

Rabinow BE. Nanosuspension in drug delivery. Nat. Rev. Drug. Discov. 3: 785–796. (2004).

Sang DY, Kim MS, Lee JC. Recrystallization of sulfathiazole and chlorpropamide using the supercritical fluid antisolvent process. J. Supercrit. Fluids. 25: 143–154 (2003).

Semalty A, Semalty M, Rawat BS, Singh D, Rawat MSM. Pharmacosomes: The lipid based novel drug delivery system. Expert. Opin. Drug Deliv. 6: 599-612 (2009a).

Semalty A, Semalty M, Singh D, Rawat MSM. Development and physicochemical evaluation of pharmacosomes of diclofenac, Acta Pharma. 59: 335–344 (2009b).

Semalty A, Semalty M, Singh D, Rawat MSM. Preparation and characterization of phospholipid complexes of naringenin for effective drug delivery. J. Incl. Phenom. Macrocycl. Chem., In press. DOI 10.1007/s10847-009-9705-8 (2009c).

Shi K, Cui F, Yu Y, Zhang L, Tao A, Cun D. Preparation and characterization of a novel insulin phospholipid complex. Asian J. Pharm. Sci. 1(3-4): 168-174 (2006).

Van JR, Botting RM. Edtors. Aspirin and other salicylates. Chapman & Hall Medical: London,; pp.245-91. (1992)

Yanyu X, Yunmei S, Zhipeng C, Quineng P. The preparation of silybin-phospholipid complex and the study on its pharmacokinetics in rats. Int. J. Pharm. 307: 77-82 (2006).

Yoo HS, Park TG. Biodegradable nanoparticles containing protein-fatty acid complex for oral delivery of salmon calcitonin. J. Pharm. Sci. 93: 488–495 (2003).