Chitosan/Casein Microparticles: Preparation, Characterization and Drug Release Studies
Microparticles carrier systems made from naturally occurring polymers based on chitosan/casein system appears to be a promising carrier for the sustained release of orally and parenteral administered drugs. In the current study we followed a microencapsulation technique based aqueous coacervation method to prepare chitosan/casein microparticles of compositions 1:1, 1:2 and 1:5 incorporated with chloramphenicol. Glutaraldehyde was used as a chemical cross-linking agent. The microparticles were prepared by aerosol method and studied by optical microscopy, infrared spectroscopy, thermo gravimetric analysis, swelling studies and drug release studies at various pH. The percentage swelling of the polymers are found to be in the order pH 4 > pH 10 > pH 7 and the increase in casein composition decrease the swelling percentage. The drug release studies also follow the above order.
[1] Morimoto Y and Fujimoto, S. "Albumin microspheres as drug carrier"
CRC Critical Reviews in Therapeutic Drug Carrier Systems, Vol. 1, No.
2, 1985, pp. 19-63.
[2] Gupta P and, Hung C. "Targeted delivery of low dose doxorubicin
hydrochloride administered via magnetic albumin microspheres in rats"
J. Microencap. Vol. 7, No. 1, 1990, pp 85-94.
[3] Chen Y, Willmott N, Anderson J and Florence A. "Comparison of
albumin and casein microspheres as a carrier for doxorubicin" J. Pharm.
Phamocol. Vol. 39, 1987, pp 978-985.
[4] Willmott N, Magee G, Cummings J, Helbert G and Smyth J.
"Doxorubicin-loaded casein microspheres: protein nature of drug
incorporation" J. Pharm. Phamocol. Vol. 44, No.12, 1992, pp 472-475.
[5] Knepp W, Jayakrishnan A, Quigg J, Sitren H, Bagnall J and Goldbergm
E. "Synthesis, properties, and intratumoral evaluation of mitoxantroneloaded
casein microspheres in Lewis lung carcinoma" J. Pharm.
Phamocol. 1993, Vol. 45, No. 10, 887-889.
[6] Latha M and Jayakrishnan A. "Albumin microspheres and
microcapsules: methodology of manufacturing techniques" J. Pharm.
Phamocol. Vol. 46, 1994, pp 858-862.
[7] Muzarelli R. "Chitin," Pergmon Press, Oxford, 1997, pp 259.
[8] Feder Jr H M, Osier C and Maderazo E G. "Chloramphenicol: a review
of its use in clinical practice" Rev. Infect. Dis. Vol. 3, No 3, 1981, pp
479-491.
[9] Austen P, Sennet S, Muzzarelli R, Jeuniaux C and Gooday G W. (Ed).
Chitin in Nature and Technology, Plenum, New York, 1986, pp 279-
286.
[10] L. Illum. "Chitosan and its use as a pharmaceutical excipient" Pharm.
Res, Vol. 15, 1998, pp 1326-1331.
[11] C. Jones, M.A. Burton and B.N. Gray. "Albumin microspheres as
vehicles for the sustained and controlled release of doxorubicin" J.
Pharm. Pharmacol. Vol. 41, 1989, pp. 813-816.
[12] Mitrevej A, Sinchaipanid N, Rungvejhavuttivittaya Y and
Kostitchaiyong V. "Multiunit controlled-Release Diclofenac Sodium
Capsules using Complex of Chitosan with Sodium Alginate or Pectin"
Pharm. Dev. Technol. 2001,Vol. 6, pp 385-392.
[13] Rinaudo M, Pavlov G and Desberiers J. "Influence of acetic acid
concentration on the solubilization of Chitosan" Polymer. Vol. 40, 1999,
pp 7029-7032.
[14] Gomori G. "Preparation of buffers for use in enzyme studies". Methods
in enzymology. Vol. 1, 1955, pp 138-146.
[15] Ahroni S M. "Synthesis characterization and theory of polymeric
networks and gels" Plenum Press, New York, 1992.
[16] Ju H. K, Kim S Y and Lee Y. M. "pH/temperature-responsive
behaviours of semi-IPN and comb-type graft hydrogels composed of
alginate and poly(N-isopropylacrylamide)" Polymer. Vol, 42, 2001, pp
6851-6857.
[17] Murali Mohan Babu G V, Prasad D. S, Narayan P. S and Raman Murthy
K. V. "New system for microencapsulation of Diclofenac Sodium by
using Gum Karaya and Chitosan" Saudi Pharm. J. Vol. 9, 2001, pp 169-
178.
[18] Bodmeir R and Paraatakul O. J. "Spherical agglomerates of waterinsoluble
drugs" J. Pharm. Sci. Vol. 78, 1989, pp 964-967.
[19] Bayomi M, Al-Suwayeh S A, El-Helw A. M and Mesned, A. F.
"Preparation of casein-chitosan microspheres containing diltiazem
hydrochloride by an aqueous coacervation Technique" Pharm. Acta.
Helv. Vol. 73, 1998, pp 187-192.
[20] Lee Y.M, Nam S.Y and Woo D.J. "Pervaporation of ionically surface
cross-linked composite membranes for water-alcohol mixtures" J. Memb.
Sci. Vol 133, 1997, pp 103-110.
[21] Silverstein R. Spectrophotometric Identification of Organic Compounds,
6th Ed., Wiley, 1998.
[22] Qu X, Wirsen A and Albertson A. C. "Effect of lactic/glycolic acid side
chains on the thermal degradation kinetics of Chitosan derivatives"
Polymer. Vol. 41, 2000, pp 4841-4847.
[23] Seong-Hoon K, Byoung-Ki L, Fangfang S, Kwangnak K, Su-Chat R,
Hong-Sung K and Jaebeom L. "Preparation of high flexible Composite
Film of Hydroxyapatite and Chitosan" Polymer Bulletin. Vol 62, No 1,
2009, pp 111-118.
[24] Gander B, Beltrami V, Gurny R and Doelker E. "Effects of the method
of drug incorporation and the size of the monolith on drug release from
cross- linked polymers" Int. J. Pharm. Vol. 58, 1990, pp 63-71.
[25] Bayomi M and El- Sayed. "Casein microbeads as a controlled parenteral
drug delivery system" Drug Dev. Ind. Pharm. Vol. 20, 1994, pp 2607-
2617.
[1] Morimoto Y and Fujimoto, S. "Albumin microspheres as drug carrier"
CRC Critical Reviews in Therapeutic Drug Carrier Systems, Vol. 1, No.
2, 1985, pp. 19-63.
[2] Gupta P and, Hung C. "Targeted delivery of low dose doxorubicin
hydrochloride administered via magnetic albumin microspheres in rats"
J. Microencap. Vol. 7, No. 1, 1990, pp 85-94.
[3] Chen Y, Willmott N, Anderson J and Florence A. "Comparison of
albumin and casein microspheres as a carrier for doxorubicin" J. Pharm.
Phamocol. Vol. 39, 1987, pp 978-985.
[4] Willmott N, Magee G, Cummings J, Helbert G and Smyth J.
"Doxorubicin-loaded casein microspheres: protein nature of drug
incorporation" J. Pharm. Phamocol. Vol. 44, No.12, 1992, pp 472-475.
[5] Knepp W, Jayakrishnan A, Quigg J, Sitren H, Bagnall J and Goldbergm
E. "Synthesis, properties, and intratumoral evaluation of mitoxantroneloaded
casein microspheres in Lewis lung carcinoma" J. Pharm.
Phamocol. 1993, Vol. 45, No. 10, 887-889.
[6] Latha M and Jayakrishnan A. "Albumin microspheres and
microcapsules: methodology of manufacturing techniques" J. Pharm.
Phamocol. Vol. 46, 1994, pp 858-862.
[7] Muzarelli R. "Chitin," Pergmon Press, Oxford, 1997, pp 259.
[8] Feder Jr H M, Osier C and Maderazo E G. "Chloramphenicol: a review
of its use in clinical practice" Rev. Infect. Dis. Vol. 3, No 3, 1981, pp
479-491.
[9] Austen P, Sennet S, Muzzarelli R, Jeuniaux C and Gooday G W. (Ed).
Chitin in Nature and Technology, Plenum, New York, 1986, pp 279-
286.
[10] L. Illum. "Chitosan and its use as a pharmaceutical excipient" Pharm.
Res, Vol. 15, 1998, pp 1326-1331.
[11] C. Jones, M.A. Burton and B.N. Gray. "Albumin microspheres as
vehicles for the sustained and controlled release of doxorubicin" J.
Pharm. Pharmacol. Vol. 41, 1989, pp. 813-816.
[12] Mitrevej A, Sinchaipanid N, Rungvejhavuttivittaya Y and
Kostitchaiyong V. "Multiunit controlled-Release Diclofenac Sodium
Capsules using Complex of Chitosan with Sodium Alginate or Pectin"
Pharm. Dev. Technol. 2001,Vol. 6, pp 385-392.
[13] Rinaudo M, Pavlov G and Desberiers J. "Influence of acetic acid
concentration on the solubilization of Chitosan" Polymer. Vol. 40, 1999,
pp 7029-7032.
[14] Gomori G. "Preparation of buffers for use in enzyme studies". Methods
in enzymology. Vol. 1, 1955, pp 138-146.
[15] Ahroni S M. "Synthesis characterization and theory of polymeric
networks and gels" Plenum Press, New York, 1992.
[16] Ju H. K, Kim S Y and Lee Y. M. "pH/temperature-responsive
behaviours of semi-IPN and comb-type graft hydrogels composed of
alginate and poly(N-isopropylacrylamide)" Polymer. Vol, 42, 2001, pp
6851-6857.
[17] Murali Mohan Babu G V, Prasad D. S, Narayan P. S and Raman Murthy
K. V. "New system for microencapsulation of Diclofenac Sodium by
using Gum Karaya and Chitosan" Saudi Pharm. J. Vol. 9, 2001, pp 169-
178.
[18] Bodmeir R and Paraatakul O. J. "Spherical agglomerates of waterinsoluble
drugs" J. Pharm. Sci. Vol. 78, 1989, pp 964-967.
[19] Bayomi M, Al-Suwayeh S A, El-Helw A. M and Mesned, A. F.
"Preparation of casein-chitosan microspheres containing diltiazem
hydrochloride by an aqueous coacervation Technique" Pharm. Acta.
Helv. Vol. 73, 1998, pp 187-192.
[20] Lee Y.M, Nam S.Y and Woo D.J. "Pervaporation of ionically surface
cross-linked composite membranes for water-alcohol mixtures" J. Memb.
Sci. Vol 133, 1997, pp 103-110.
[21] Silverstein R. Spectrophotometric Identification of Organic Compounds,
6th Ed., Wiley, 1998.
[22] Qu X, Wirsen A and Albertson A. C. "Effect of lactic/glycolic acid side
chains on the thermal degradation kinetics of Chitosan derivatives"
Polymer. Vol. 41, 2000, pp 4841-4847.
[23] Seong-Hoon K, Byoung-Ki L, Fangfang S, Kwangnak K, Su-Chat R,
Hong-Sung K and Jaebeom L. "Preparation of high flexible Composite
Film of Hydroxyapatite and Chitosan" Polymer Bulletin. Vol 62, No 1,
2009, pp 111-118.
[24] Gander B, Beltrami V, Gurny R and Doelker E. "Effects of the method
of drug incorporation and the size of the monolith on drug release from
cross- linked polymers" Int. J. Pharm. Vol. 58, 1990, pp 63-71.
[25] Bayomi M and El- Sayed. "Casein microbeads as a controlled parenteral
drug delivery system" Drug Dev. Ind. Pharm. Vol. 20, 1994, pp 2607-
2617.
@article{"International Journal of Biological, Life and Agricultural Sciences:55648", author = "Selvakumar Dhanasingh and Shunmuga Kumar Nallaperumal", title = "Chitosan/Casein Microparticles: Preparation, Characterization and Drug Release Studies", abstract = "Microparticles carrier systems made from naturally occurring polymers based on chitosan/casein system appears to be a promising carrier for the sustained release of orally and parenteral administered drugs. In the current study we followed a microencapsulation technique based aqueous coacervation method to prepare chitosan/casein microparticles of compositions 1:1, 1:2 and 1:5 incorporated with chloramphenicol. Glutaraldehyde was used as a chemical cross-linking agent. The microparticles were prepared by aerosol method and studied by optical microscopy, infrared spectroscopy, thermo gravimetric analysis, swelling studies and drug release studies at various pH. The percentage swelling of the polymers are found to be in the order pH 4 > pH 10 > pH 7 and the increase in casein composition decrease the swelling percentage. The drug release studies also follow the above order.
", keywords = "Chitosan/casein micro particles, chloramphenicol, drug release, microencapsulation.", volume = "4", number = "8", pages = "572-5", }
