Development of Polymeric Blend Microspheres from Chitosan-Hydroxypropylmethyl Cellulose for Controlled Release of an Anti-Cancer Drug

다국어 초록 (Multilingual Abstract)

Chitosan (CS) and hydroxypropylmethyl cellulose (HPMC) blend microspheres were prepared by water-in-oil emulsion technique and were loaded with an anti-cancer drug 5-fluorouracil (5-FU). CS-HPMC microspheres were characterized by Fourier transform infrared spectroscopy to confirm the cross-linking reaction. Scanning electron microscopy (SEM) was also used to assess the surface morphology of particles prepared. The quantity of release of 5-FU from the microspheres have been studied in terms of blend composition and amount of cross-linking agent. Differential scanning calorimetry and X-ray diffraction techniques indicated a uniform distribution of 5-FU particles in microspheres, whereas SEM suggested the spherical structure of the microspheres with slight rough surface. The in vitro drug release indicated that the particle size and release kinetics depend upon blend composition, amount of cross-linking agent used and amount of 5-FU present in the microspheres.

참고문헌 (Reference)

1 Peppas, N. A., 11 : 1-35, 1993

2 Holgado, M. A., 118 : 151-, 1995

3 Miyazaki, S., "The Use of Chitin and Chitosan as Drug Carriers" 29 : 3067-3069, 1981

4 Peppas, L. B., "The Equilibrium Swelling Behavior of Porous and Non-Porous Hydrogels. In Absorbent Polymer Technology" Elsevier 67-102, 1990

5 Kahtani Ahmed, A. L., "Synthesis and Characterization of Chitosan-Based pHSensitive Semi-Interpenetrating Network Microspheres for Controlled Release of Diclofenac Sodium" 699-706, 2009

6 Hos, W. M., "Sustained Release of Indomethacin from Chitosan Granules" 33 : 3986-3992, 1985

7 Chowhan, Z. T., "Role of Binders in Moisture-Induced Hardness Increase in Compressed Tablets and Its Effect on in Vitro Disintegration and Dissolution" 69 : 1-4, 1980

8 Cadee, J. A., "Release of Recombinant Human Interleukin- 2 from Dextran-Based Hydrogels" 78 : 1-13, 2002

9 Ford, J. L., "Propranolol Hydrochloride and Aminophylline Release from Matrix Tablets Containing Hydroxypropylmethylcellulose" 24 : 339-350, 1985

10 Van, T. N., "Production of High-Quality Chitin and Chitosan from Preconditioned Shrimp Shells" 81 (81): 1113-1118, 2006

11 Cuna, M., "Preparation and in Vivo Evaluation of Mucoadhesive Microparticles Containing Amoxycillin–-Resin Complexes for Drug Delivery to the Gastric Mucosa" 51 : 199-205, 2001

12 Peppas, L. B., "Preparation and Characterization of Crosslinked Hydrophilic Networks. In Absorbent Polymer Technology" Elsevier 45-66, 1990

13 Cory, B., "Precise Control of PLG Microsphere Size Provides Enhanced Control of Drug Release Rate" 82 : 137-147, 2002

14 Tahara, K., "Overall Mechanism Behind Matrix Sustained Release(SR) Tablets Prepared with Hydroxypropyl Methylcellulose 2910" 35 : 59-66, 1995

15 Salsa, T., "Oral Controlled-Release Dosage Forms. I. Cellulose Ether Polymers in Hydrophilic Matrices" 23 : 929-938, 1997

16 Ajit, P. R., "Novel Interpenetrating Polymer Network Microspheres of Chitosan and Methylcellulose for Controlled Release of Theophylline" 69 : 678-687, 2007

17 Siepmann, J., "Modeling of Drug Release from Delivery Systems Based on Hydroxypropyl Methylcellulose (HPMC)" 48 : 139-157, 2001

18 Sudha, C. A., "Interpenetrating Polymer Network Blend Microspheres of Chitosan and Hydroxyethyl Cellulose for Controlled Release of Isoniazid" 47 : 171-179, 2010

19 Campos-Aldrete, M. E., "Influence of the Viscosity Degree and the Particle Size of HPMC on Metronidazole Release from Matrix Tablets" 43 : 173-178, 1997

20 Perez-Marcos, B., "Influence of pH on the Release of Propranolol Hydrochloride from Matrices Containing Hydroxypropylmethyl Cellulose K4M and Carbopol 974" 85 : 330-334, 1996

21 Lim, S. T., "In Vivo Evaluation of Novel Hyaluronan/Chitosan Microparticulate Delivery Systems for the Nasal Delivery of Gentamicin in Rabbits" 231 : 73-82, 2002

22 Ford, J. L., "Formulation of Sustained Release Promethazine Hydrochloride Tablets Using Hydroxypropylmethylcellulose Matrices" 24 : 327-338, 1985

23 Sawayanagi, Y., "Enhancement of Dissolution Properties of Prednisolone from Ground Mixtures with Chitin or Chitosan" 31 : 2507-2509, 1983

24 Sawayanagi, Y., "Directly Compressed Tablets Containing Chitin or Chitosan in Addition to Lactose or Potato Starch" 30 : 2935-2940, 1982

25 Ryoichi, M., "Development of Oral Controlled Release Preparations, a PVA Swelling Controlled Release System (SCRS). II. In Vitro and in Vivo Evaluation" 68 : 115-120, 2000

26 Krogel, I., "Developemnt of a Multifunctional Matrix Drug Delivery System Surrounded by an Impermeable Cylinder" 61 : 43-50, 1999

27 Chowdary, K. P. R., "Design and in Vitro and in Vivo Evaluation of Mucoadhesive Microcapsules of Glipizide for Oral Controlled Release: A Technical Note" 4 : 87-92, 2003

28 Krishna Rao, K. S. V., "Controlled Release of Ibuprofen and Diclofenac Sodium through Beads of Alginate and Hydroxyethyl Cellulose Blends" 102 : 5708-5718, 2006

29 Sezer, A. D., "Comparison on In Vitro Characterization of Fucospheres and Chitosan Microspheres Encapsulated Plasmid DNA (pGM-CSF): Formulation Design and Release Characteristics" 1193-1199, 2009

30 Vazquez, M. J., "Atenlol Release from Hydrophilic Matrix Tablets with Hydroxyl Propylmethyl Cellulose (HPMC) Mixtures as Gelling Agent: Effects of Viscosity of the HPMC Mixture" 4 : 39-48, 1996

31 Pillay, V., "A Novel Approach for Constant Rate Delivery of Highly Soluble Bioactives from a Simple Monolithic System" 67 : 67-78, 2000