Characterization and Antimicrobial Activity of N-Methyl-2-pyrrolidone-loaded Ethylene Oxide-Propylene Oxide Block Copolymer Thermosensitive Gel

Overview

Journal Indian J Pharm Sci

Specialty Pharmacy

Date 2013 Jun 27

PMID 23798774

Citations 14

Authors

T Phaechamud

J Mahadlek

J Charoenteeraboon

S Choopun

Affiliations

Soon will be listed here.

Abstract

The purpose of this study is to investigate the effects of N-methyl-2-pyrrolidone on the thermosensitive properties of aqueous ethylene oxide-propylene oxide block copolymer (Lutrol(®) F127) system. Due to the aqueous solubility enhancement and biocompatibility, N-methyl-2-pyrrolidone is an interesting solubilizer for the poorly water soluble drugs to be incorporated in the Lutrol(®) F127 system. Effect of N-methyl-2-pyrrolidone on physicochemical properties of Lutrol(®) F127 system was investigated using appearance, pH, gelation, gel melting temperature and rheology. The antimicrobial activity of the thermosensitive N-methyl-2-pyrrolidone gel was also tested. Lower N-methyl-2-pyrrolidone amount (≤30%w/w) could shift the sol-gel transition to a lower temperature but the gel-sol transition was shifted to a higher temperature. Higher N-methyl-2-pyrrolidone (≥40%w/w) could shift both sol-gel and gel-sol transitions of the system to a lower temperature. The amount of N-methyl-2-pyrrolidone >60% w/w could reverse the phase of the Lutrol(®) F127 system to non-newtonian flow at 4° and Newtonian flow at high temperature. Aqueous Lutrol(®) F127 system containing N-methyl-2-pyrrolidone exhibited antimicrobial activities against Staphylococcus aureus, Escherichia coli and Candida albicans with the N-methyl-2-pyrrolidone in a dose-dependent manner.

Citing Articles

New Nanobioceramics Based on Hydroxyapatite for Biomedical Applications: Stability and Properties.

Ciobanu C, Predoi D, Iconaru S, Negrila C, Leduc D, Ghegoiu L Nanomaterials (Basel). 2025; 15(3).

PMID: 39940201 PMC: 11820604. DOI: 10.3390/nano15030224.

Cellulose Acetate Butyrate-Based In Situ Gel Comprising Doxycycline Hyclate and Metronidazole.

Khaing E, Lertsuphotvanit N, Thammasut W, Rojviriya C, Chansatidkosol S, Phattarateera S Polymers (Basel). 2025; 16(24.

PMID: 39771329 PMC: 11728690. DOI: 10.3390/polym16243477.

Moxifloxacin HCl -loaded Cellulose Acetate Butylate In Situ Forming Gel for Periodontitis Treatment.

Thammasut W, Rojviriya C, Chaiya P, Phaechamud T, Limsitthichaikoon S AAPS PharmSciTech. 2024; 25(7):242.

PMID: 39402367 DOI: 10.1208/s12249-024-02960-1.

Process Development for Fabricating 3D-Printed Polycaprolactone-Infiltrated Hydroxyapatite Bone Graft Granules: Effects of Infiltrated Solution Concentration and Agitating Liquid.

Thammarakcharoen F, Srion A, Suvannapruk W, Chokevivat W, Limtrakarn W, Suwanprateeb J Biomedicines. 2024; 12(9).

PMID: 39335674 PMC: 11429199. DOI: 10.3390/biomedicines12092161.

Fluconazole-Loaded Ibuprofen In Situ Gel-Based Oral Spray for Oropharyngeal Candidiasis Treatment.

Khaing E, Senarat S, Jitrangsri K, Phaechamud T AAPS PharmSciTech. 2024; 25(5):89.

PMID: 38641711 DOI: 10.1208/s12249-024-02804-y.

References

Shin S, Cho C . Physicochemical characterizations of piroxicam-poloxamer solid dispersion. Pharm Dev Technol. 1998; 2(4):403-7. DOI: 10.3109/10837459709022639. View

Schmolka I . Artificial skin. I. Preparation and properties of pluronic F-127 gels for treatment of burns. J Biomed Mater Res. 1972; 6(6):571-82. DOI: 10.1002/jbm.820060609. View

Polson A, Garrett S, Stoller N, Bandt C, Hanes P, Killoy W . Multi-center comparative evaluation of subgingivally delivered sanguinarine and doxycycline in the treatment of periodontitis. II. Clinical results. J Periodontol. 1997; 68(2):119-26. DOI: 10.1902/jop.1997.68.2.119. View

Yong C, Choi J, Quan Q, Rhee J, Kim C, Lim S . Effect of sodium chloride on the gelation temperature, gel strength and bioadhesive force of poloxamer gels containing diclofenac sodium. Int J Pharm. 2001; 226(1-2):195-205. DOI: 10.1016/s0378-5173(01)00809-2. View

Scherlund M, Malmsten M, Holmqvist P, Brodin A . Thermosetting microemulsions and mixed micellar solutions as drug delivery systems for periodontal anesthesia. Int J Pharm. 1999; 194(1):103-16. DOI: 10.1016/s0378-5173(99)00366-x. View

Maheshwari M, Miglani G, Mali A, Paradkar A, Yamamura S, Kadam S . Development of tetracycline-serratiopeptidase-containing periodontal gel: formulation and preliminary clinical study. AAPS PharmSciTech. 2006; 7(3):76. PMC: 2750518. DOI: 10.1208/pt070376. View

Rhee Y, Shin Y, Park C, Chi S, Park E . Effect of flavors on the viscosity and gelling point of aqueous poloxamer solution. Arch Pharm Res. 2007; 29(12):1171-8. DOI: 10.1007/BF02969310. View

Juhasz J, Lenaerts V, Raymond P, Ong H . Diffusion of rat atrial natriuretic factor in thermoreversible poloxamer gels. Biomaterials. 1989; 10(4):265-8. DOI: 10.1016/0142-9612(89)90103-8. View

Dimitrova E, Bogdanova S, Mitcheva M, Tanev I, MINKOV E . Development of model aqueous ophthalmic solution of indomethacin. Drug Dev Ind Pharm. 2001; 26(12):1297-301. DOI: 10.1081/ddc-100102312. View

10.

Ravivarapu H, Moyer K, Dunn R . Sustained suppression of pituitary-gonadal axis with an injectable, in situ forming implant of leuprolide acetate. J Pharm Sci. 2000; 89(6):732-41. DOI: 10.1002/(SICI)1520-6017(200006)89:6<732::AID-JPS4>3.0.CO;2-D. View

11.

Kranz H, Bodmeier R . Structure formation and characterization of injectable drug loaded biodegradable devices: in situ implants versus in situ microparticles. Eur J Pharm Sci. 2008; 34(2-3):164-72. DOI: 10.1016/j.ejps.2008.03.004. View

12.

Barichello J, Morishita M, Takayama K, Chiba Y, Tokiwa S, Nagai T . Enhanced rectal absorption of insulin-loaded Pluronic F-127 gels containing unsaturated fatty acids. Int J Pharm. 1999; 183(2):125-32. DOI: 10.1016/s0378-5173(99)00090-3. View

13.

Choi H, Lee M, Kim M, Kim C . Effect of additives on the physicochemical properties of liquid suppository bases. Int J Pharm. 1999; 190(1):13-9. DOI: 10.1016/s0378-5173(99)00225-2. View

14.

Maheshwari M, Paradkar A, Yamamura S, Kadam S . Preparation and characterization of pluronic-colloidal silicon dioxide composite particles as liquid crystal precursor. AAPS PharmSciTech. 2007; 7(4):92. PMC: 2750329. DOI: 10.1208/pt070492. View

15.

Koizumi A, Fujii M, Kondoh M, Watanabe Y . Effect of N-methyl-2-pyrrolidone on skin permeation of estradiol. Eur J Pharm Biopharm. 2004; 57(3):473-8. DOI: 10.1016/j.ejpb.2003.12.006. View

16.

Eberlein-Konig B, Schafer T, Huss-Marp J, Darsow U, Mohrenschlager M, Herbert O . Skin surface pH, stratum corneum hydration, trans-epidermal water loss and skin roughness related to atopic eczema and skin dryness in a population of primary school children. Acta Derm Venereol. 2000; 80(3):188-91. DOI: 10.1080/000155500750042943. View

17.

Akhter S, Barry B . Absorption through human skin of ibuprofen and flurbiprofen; effect of dose variation, deposited drug films, occlusion and the penetration enhancer N-methyl-2-pyrrolidone. J Pharm Pharmacol. 1985; 37(1):27-37. DOI: 10.1111/j.2042-7158.1985.tb04926.x. View

18.

Pandit , Trygstad , Croy , Bohorquez , KOCH . Effect of Salts on the Micellization, Clouding, and Solubilization Behavior of Pluronic F127 Solutions. J Colloid Interface Sci. 2000; 222(2):213-220. DOI: 10.1006/jcis.1999.6628. View