Pharmaceutical Microencapsulation Technology for Development of Controlled Release Drug Delivery systems
This article demonstrated development of
controlled release system of an NSAID drug, Diclofenac
sodium employing different ratios of Ethyl cellulose.
Diclofenac sodium and ethyl cellulose in different proportions
were processed by microencapsulation based on phase
separation technique to formulate microcapsules. The
prepared microcapsules were then compressed into tablets to
obtain controlled release oral formulations. In-vitro evaluation
was performed by dissolution test of each preparation was
conducted in 900 ml of phosphate buffer solution of pH 7.2
maintained at 37 ± 0.5 °C and stirred at 50 rpm. At predetermined
time intervals (0, 0.5, 1.0, 1.5, 2, 3, 4, 6, 8, 10, 12,
16, 20 and 24 hrs). The drug concentration in the collected
samples was determined by UV spectrophotometer at 276 nm.
The physical characteristics of diclofenac sodium
microcapsules were according to accepted range. These were
off-white, free flowing and spherical in shape. The release
profile of diclofenac sodium from microcapsules was found to
be directly proportional to the proportion of ethylcellulose and
coat thickness. The in-vitro release pattern showed that with
ratio of 1:1 and 1:2 (drug: polymer), the percentage release of
drug at first hour was 16.91 and 11.52 %, respectively as
compared to 1:3 which is only 6.87 % with in this time. The
release mechanism followed higuchi model for its release
pattern. Tablet Formulation (F2) of present study was found
comparable in release profile the marketed brand Phlogin-SR,
microcapsules showed an extended release beyond 24 h.
Further, a good correlation was found between drug release
and proportion of ethylcellulose in the microcapsules.
Microencapsulation based on coacervation found as good
technique to control release of diclofenac sodium for making
the controlled release formulations.
[1] H. Arabi, S. A. Hashemi, and M. Fooladi, Microencapsulation of
allupurinol by solvent evaporation and controlled release investigation
of drugs. Journal of Microencapsulation; 1996, 13: 527-535.
[2] P. B. Deasy, Microencapsulation and related drug processes, (New Yark:
Marcel Dekker) 1984, pp 16-20.
[3] G. Cheng, F. An, M. J. Zou, J. Sun, X. H. Hao, Y. X. He, Time- and pHdependent
colon-specific drug delivery for orally administered
diclofenac sodium and 5-aminosalicylic acid; World J Gastroenterol
2004, 10 (12):1769-1774
[4] A. Kristl, M. Bogataj, A. Mrhar and F. Kozjek, Preparation and
Evaluation of ethyl cellulose Microcapsules with Bacampicillin. Drug
Develop Ind Pharm; 1991, 18 (8):1109-30.
[5] L. Lachman, H. A. Lieberman, and J. I. Kanig, the Theory and Practice
of Industrial Pharmacy. 2nd ed. Philadelphia; Lea & Febiger 1986,
pp.412-429.
[6] J W. J. Lin and T. L. Wu, Modification of the initial release of a highly
water soluble drug from Ethylcellulose microspheres, Journal of
Microencapsulation; 1999, 16: 639-644.
[7] R. W. Mendes and S. B. Roy, tabletting excipients. Part 11. Pharm
Technlo, 1978, 3-63.
[8] R. N. Saha, C. Sajeev, and Sahoo J, A comparative study of controlled
release matrix tablets of Diclofenac sodium, Ciprofloxacin
hydrochloride and Theophylline. Drug delivery; 2001, 8: 149-154.
[9] C. Sajeev, R. Pravin, D. Jadhav, K. Ravishankar and R. N. Saha,
Determination of DFS in pharmaceutical formulations by UV
spectrophotometry and liquid chromatography. Analytica Chimica Acta;
2002, (463): 207-217.
[10] J S. P. Sanghvi and J. G. Nairn, Phase diagram studies for
Microencapsulation of pharmaceuticals using cellulose trimellitate. J
Pharm Sci; 1991, 80 (4):349-8.
[11] M. Saravanan, K. Bhaskar, R. G. Srinivasa and M. D. Dhanaraju,
Ibuprofen loaded Ethylcellulose /polystyrene microspheres. Approaches
to get prolong drug release with reduce burst effect and low
Ethylcellulose contents. J Microencapsul; 2003, (20): 289-302.
[12] B. Simon, Microencapsulation: Methods and Industrial Application,
Second Edition, Chapter 4 Microencapsulation Techniques for
Parenteral Depot Systems and T heir Application in the Pharmaceutical
Industry, authors, Claudia Packhauser Nina Seidel , Julia Schnieders ,
Thomas Kissel , and Sascha Maretschek, 2006, 99-122 ISBN: 978-0-
8247-2317-0
[13] K. D. Sudip, In-Vitro dissolution profile of the theophylline loaded
Ethylcellulose microsphers prepared by emulsification solvent
evaporation. Drug Development and Industrial Pharmacy; 1991, 17:
2521-2528.
[14] S. J. Svinsson, and Kristmunsdottir, Naproxen Microcapsules:
Preparation and In-Vitro characterization. Int J Pharm, 1992, (82):129-
33.
[15] The British pharmacopoeia, (2004) Vol. I; 861-862
[16] C. Zinutti, F. Kedzierewicz, M. Hoffman, and P. Mancent, Preparation
and characterization of Ethylcellulose microspheres containing 5-
fluorouracil. Journal of Microencapsulation; 1994, 11: 555-563.
[1] H. Arabi, S. A. Hashemi, and M. Fooladi, Microencapsulation of
allupurinol by solvent evaporation and controlled release investigation
of drugs. Journal of Microencapsulation; 1996, 13: 527-535.
[2] P. B. Deasy, Microencapsulation and related drug processes, (New Yark:
Marcel Dekker) 1984, pp 16-20.
[3] G. Cheng, F. An, M. J. Zou, J. Sun, X. H. Hao, Y. X. He, Time- and pHdependent
colon-specific drug delivery for orally administered
diclofenac sodium and 5-aminosalicylic acid; World J Gastroenterol
2004, 10 (12):1769-1774
[4] A. Kristl, M. Bogataj, A. Mrhar and F. Kozjek, Preparation and
Evaluation of ethyl cellulose Microcapsules with Bacampicillin. Drug
Develop Ind Pharm; 1991, 18 (8):1109-30.
[5] L. Lachman, H. A. Lieberman, and J. I. Kanig, the Theory and Practice
of Industrial Pharmacy. 2nd ed. Philadelphia; Lea & Febiger 1986,
pp.412-429.
[6] J W. J. Lin and T. L. Wu, Modification of the initial release of a highly
water soluble drug from Ethylcellulose microspheres, Journal of
Microencapsulation; 1999, 16: 639-644.
[7] R. W. Mendes and S. B. Roy, tabletting excipients. Part 11. Pharm
Technlo, 1978, 3-63.
[8] R. N. Saha, C. Sajeev, and Sahoo J, A comparative study of controlled
release matrix tablets of Diclofenac sodium, Ciprofloxacin
hydrochloride and Theophylline. Drug delivery; 2001, 8: 149-154.
[9] C. Sajeev, R. Pravin, D. Jadhav, K. Ravishankar and R. N. Saha,
Determination of DFS in pharmaceutical formulations by UV
spectrophotometry and liquid chromatography. Analytica Chimica Acta;
2002, (463): 207-217.
[10] J S. P. Sanghvi and J. G. Nairn, Phase diagram studies for
Microencapsulation of pharmaceuticals using cellulose trimellitate. J
Pharm Sci; 1991, 80 (4):349-8.
[11] M. Saravanan, K. Bhaskar, R. G. Srinivasa and M. D. Dhanaraju,
Ibuprofen loaded Ethylcellulose /polystyrene microspheres. Approaches
to get prolong drug release with reduce burst effect and low
Ethylcellulose contents. J Microencapsul; 2003, (20): 289-302.
[12] B. Simon, Microencapsulation: Methods and Industrial Application,
Second Edition, Chapter 4 Microencapsulation Techniques for
Parenteral Depot Systems and T heir Application in the Pharmaceutical
Industry, authors, Claudia Packhauser Nina Seidel , Julia Schnieders ,
Thomas Kissel , and Sascha Maretschek, 2006, 99-122 ISBN: 978-0-
8247-2317-0
[13] K. D. Sudip, In-Vitro dissolution profile of the theophylline loaded
Ethylcellulose microsphers prepared by emulsification solvent
evaporation. Drug Development and Industrial Pharmacy; 1991, 17:
2521-2528.
[14] S. J. Svinsson, and Kristmunsdottir, Naproxen Microcapsules:
Preparation and In-Vitro characterization. Int J Pharm, 1992, (82):129-
33.
[15] The British pharmacopoeia, (2004) Vol. I; 861-862
[16] C. Zinutti, F. Kedzierewicz, M. Hoffman, and P. Mancent, Preparation
and characterization of Ethylcellulose microspheres containing 5-
fluorouracil. Journal of Microencapsulation; 1994, 11: 555-563.
@article{"International Journal of Medical, Medicine and Health Sciences:64372", author = "Mahmood Ahmad and Asadullah Madni and Muhammad Usman and Abubakar Munir and Naveed Akhtar and Haji M. Shoaib Khan", title = "Pharmaceutical Microencapsulation Technology for Development of Controlled Release Drug Delivery systems", abstract = "This article demonstrated development of
controlled release system of an NSAID drug, Diclofenac
sodium employing different ratios of Ethyl cellulose.
Diclofenac sodium and ethyl cellulose in different proportions
were processed by microencapsulation based on phase
separation technique to formulate microcapsules. The
prepared microcapsules were then compressed into tablets to
obtain controlled release oral formulations. In-vitro evaluation
was performed by dissolution test of each preparation was
conducted in 900 ml of phosphate buffer solution of pH 7.2
maintained at 37 ± 0.5 °C and stirred at 50 rpm. At predetermined
time intervals (0, 0.5, 1.0, 1.5, 2, 3, 4, 6, 8, 10, 12,
16, 20 and 24 hrs). The drug concentration in the collected
samples was determined by UV spectrophotometer at 276 nm.
The physical characteristics of diclofenac sodium
microcapsules were according to accepted range. These were
off-white, free flowing and spherical in shape. The release
profile of diclofenac sodium from microcapsules was found to
be directly proportional to the proportion of ethylcellulose and
coat thickness. The in-vitro release pattern showed that with
ratio of 1:1 and 1:2 (drug: polymer), the percentage release of
drug at first hour was 16.91 and 11.52 %, respectively as
compared to 1:3 which is only 6.87 % with in this time. The
release mechanism followed higuchi model for its release
pattern. Tablet Formulation (F2) of present study was found
comparable in release profile the marketed brand Phlogin-SR,
microcapsules showed an extended release beyond 24 h.
Further, a good correlation was found between drug release
and proportion of ethylcellulose in the microcapsules.
Microencapsulation based on coacervation found as good
technique to control release of diclofenac sodium for making
the controlled release formulations.", keywords = "Diclofenac sodium, Microencapsulationtechnology, Ethylcellulose, In-Vitro Release Profile", volume = "5", number = "3", pages = "133-4", }