Formulation and in vitro characterization of alginate microspheres loaded with diloxanide furoate for colon- specific drug delivery

Shailendra Shukla, Deepak Jain, Kavita Verma


The aim of the research work was to develop cyst–targeted alginates microspheres of diloxanide furoate (DF) for the effective treatment of amoebiasis. Calcium alginates microspheres of DF were prepared using emulsification method using calcium chloride as a cross-linking agent. Alginate is a natural polysaccharide found in brown algae. Alginates are widely used in the food and pharmaceutical industries and have been employed as a matrix for the entrapment of drugs, macromolecules and biological cells. Alginate microspheres produced by the emulsification method using calcium chloride.
Formulations were characterized for particle size and shape, surface morphology, entrapment efficiency, and in vitro drug release in simulated gastrointestinal fluids. XRD and differential scanning calorimetery were used to confirm successful
entrapment of DF into the alginates microspheres. All the microsphere formulations showed good % drug entrapment (73.82±1.99). Calcium alginate retarded the release of DF at low pH (1.2 and 4.5) and released microspheres slowly at pH 7.4 in the colon without colonic enzymes.

Full Text:



Macfarlane GT, Hay S, Macfarlane S, Gibson GR. Effect of different

carbohydrates on growth polysaccharidases and glycosidase production

of Bacteroides ovatus in batch and continuous culture. J Appl Bacteriol


Jain SK, Rai G, Saraf DK, Agrawal GP. The preparation and evaluation

of albendazole microspheres for colonic delivery. Pharmaceutical


Davis SS. Overcoming barriers to the oral administration of peptide

drugs. Trends Pharma Sci 1990;11:353-5.

Swords R, Cantey RJ. Amoebiasis. Gastroent Clin 2002;25:28-9.

Vaidya A, Jain A, Khare P, Agrawal RK, Jain SK. Metronidazole loaded

pectin microspheres for colon targeting. J Pharm Sci 2009;98:4229-36.

Gregoriadis G, Florence AT. Liposomes in drug delivery. Clinical,

diagnostic and ophthalmic potential. Drugs 1993;145:15-28.

He P, Davis SS, Illum L. In-vitro evaluation of the mucoadhesive

properties of chitosan microspheres. Int J Pharm 2005;297:172-9.

Draget KI, Skjak-Braek G, Smidsrød O. Alginate based new materials.

Int J Biol Macromol 1997;21:47-55.

Esposito E, Cortesi R, Luca G, Nastruzzi C. Pectin-Based Microspheres:

A Preformulatory Study. Ann NY Acad Sci 2001;944:160-79.

Srimornsak P. Investigation of pectin as a carrier for oral delivery of

proteins using calcium pectinate gel beads. Int J Pharm 1998;169:213-20.

Srimornsak P, Nunthanid J. Calcium pectinate gel beads for controlled

release drug delivery: I. Preparation and in-vitro release studies. Int J

Pharm 1998;160:207-12.

Durig T, Fassihi R. Guar based monolithic matrix system: Effect of

non-ionizable substances and excipients on gel dynamics and release

kinetics. J Control Rel 2002;80:45-56.

Haug A, Larsen B. Quantitative determination of the uronic acid

composition of alginates. Acta Chem Scand 1962;16:1908-18.

Haug A, Larsen B, Smidsrød O. Studies on the sequence of uronic acid residues in alginic acid. Acta Chem Scand 1967;21:691-704.

Kim CK, Lee EJ. The controlled release of blue dextran from alginates

beads. Int J Pharm 1992;79:11-9.

Yotsuyanagi T, Ohkubo T, Ohhashi T, Ikeda K, Calcium-induced gelatin

of alginic acid and pH sensitive reswelling of dried gels. Chem Pharm

Bull 1987;35:1555-63.

Dubey MP, Gupta PS, Chutanni HK. Entamide furoate in the treatment

of intestinal amoebiasis. J Trop Med Hyg 1965;68:63-6.

Maia JL, Santana MH, Re MI. The effect of some processing conditions

on the characteristics of biodegradable microspheres obtained by an

emulsion solvent evaporation process. Braz J Chem Eng 2004;21:1-12.

Anande NM, Jain SK, Jain NK. Con-A conjugated mucoadhesive

microspheres for the colonic delivery of Diloxanide furoate. Int J

Pharma 2008;359:182-9.

Abraham S, Srinath MS. Development of modified pulsincap drug

delivery system of metronidazole for drug targeting. Indian J Pharm

Sci 2007;69:24-7.

Bigucci F, Luppi B, Monacoa L, Cerchiarab T, Zecchi V. Pectin-based

microspheres for colon-specific delivery of vancomycin. J Pharm

Pharmacol 2009;61:41-6.

Calis S, Arica B, Kas HS, Hincal AA. 5-Fluorouracil-loaded alginate

microspheres in chitosan gel for local therapy of breast cancer. In:

Muzzarelli RA, Muzzarelli C, editors. Chitosan in Pharmacy and

Chemistry. Grottammare, Italy: Atec; 2002. p. 65-9.

Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted

drug delivery systems. J Pharm Pharmaceut Sci 2003;6:33-66.

Dashora A, Jain CP. Development and characterization of pectin-

prednisolone microspheres for colon targeted delivery. Int J Chem

Tech Res 2009;1:751-7.

Kawashima Y, Niwa T, Takeuchi H, Hino T, Ito Y. Preparation of multiple

unit hollow microspheres (microballoons) with acrylic resin containing

tranilast and their drug release characteristics (in vitro) and floating

behavior (in vivo). J Control Release 1991;16:279-90.

Rai G, Jain SK, Agrawal S, Pancholi SS, Agrawal GP. Chitosan

hydrochloride based microspheres of albendazole for colonic drug

delivery. Pharmazie 2005;60:131-4.

Pongpaibul Y, Price JC, Whitworth CW. Preparation and evaluation of

controlled release indomethacin microspheres. Drug Dev Ind Pharm




  • There are currently no refbacks.