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Abstract
Purpose: To investigate the solubilization of poorly water-soluble non-steroidal anti-inflammatory drugs (NSAIDs) in N-benzyl-N,O-succinyl chitosan (BSCS) polymeric micellesMethods: BSCS was synthesized by reductive amination and succinylation, respectively. NSAIDs; meloxicam (MX), piroxicam (PRX), ketoprofen (KP) and indomethacin (IND) were entrapped in the hydrophobic inner cores by evaporation method. The effects of drug structure on loading efficiency, particle size and surface charge of micelles were investigated.Results: The critical micelle concentration of BSCS micelles was 0.0385 mg/mL and cytotoxicity on Caco-2 cells depends on the polymer concentration (IC50 = 3.23 ± 0.08 mg/mL). BSCS micelles were able to entrap MX, PRX, KP and IND and also improve the solubility of drugs. Drug loading efficiency was highly dependent on the drug molecules. The drug loading capacity of these BSCS micelles was in the following rank order: KP (282.9 μg/mg) > PRX (200.8 μg/mg) > MX (73.7 μg/mg) > IND (41.2 μg/mg). The highest loading efficiency was observed in KP-loaded BSCS micelles due to the attractive force between phenyl groups of KP and benzyl groups of the polymer. Particle size and surface charge were in the range of 312 - 433 nm and -38 to -41 mV, respectively.Conclusion: BSCS copolymer presents desirable attributes for enhancing the solubility of hydrophobic drugs. Moreover, BSCS polymeric micelles might be beneficial carrier in a drug delivery system.Keywords: BSCS, polymeric micelles, solubilization, non-steroidal anti-inflammatory drugs
Highlights
One-third of the drugs identified are poorly water soluble, which is one of the important hindrances for successful development and the therapy of the orally administered drug effective [1,2]
Drug-incorporated polymeric micelles can be formulated from amphiphilic copolymer with entrapped drug in the hydrophobic inner core and hydrophilic segment surrounding aqueous medium to stabilize the micelles
The N-benzylation of CS occurred through the corresponding Schiff base intermediate, the N,O-succinylation of Biopharmaceutics Classification System (BCS) was performed by reacting with succinic anhydride in DMF at 100 °C
Summary
One-third of the drugs identified are poorly water soluble, which is one of the important hindrances for successful development and the therapy of the orally administered drug effective [1,2]. The core-shell polymeric micelles is an alternative technique to dissolve hydrophobic drugs. Drug-incorporated polymeric micelles can be formulated from amphiphilic copolymer with entrapped drug in the hydrophobic inner core and hydrophilic segment surrounding aqueous medium to stabilize the micelles. There has been great importance in the use of polymeric micelles as drug carriers [5]. The successful of hydrophobic drugs loaded into polymeric micelles can solubilize 10-5000 fold in aqueous solutions [6]
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