A B S T R A C T Background:Microencapsulation is a useful method to prolong a drug release from dosage forms and to reduce its adverse effect (1) among various available methods. The microencapsulation of hydrophilic active ingredients requires the use of a polar dispersing phase such as a mineral oil. Acetone/paraffin systems are conventionally used. Objectives: The current study aimed to investigate two different microencapsulation techniques comparatively, water in oil in oil (w/o/o) and oil in oil (o/o), for theophylline (TH) loaded ethylcellulose (EC), cellulose acetate butyrate (CAB), Eudragit RS and RL microspheres with regard to loading efficiency, release and degradation kinetics. Materials and Methods: Microspheres were prepared by the emulsification method by solvent diffusion/evaporation technique and different polymers which were incorporated into microspheres to control the release rate of drug. Theophylline (TH) was chosen as a model drug. The emulsion technique was investigated for to prepare theophylline microparticles. EC and CAB and acrylatemethacrylate copolymer corresponding to the above ratios were selected as microparticles wall materials. The effects of type polymers on the physical characteristics and dissolution of the microparticles were also studied. However, the TH loading efficiency (for w/o/o emulsion about 90.64% and o/o emulsion about 73.90/5 to 95.90%) and the TH release kinetics were influenced by the microencapsulation technique. Results:The results demonstrated that the o/o microspheres (containing of CAB) was most appropriate, providing a high encapsulation efficiency (95.90%) and low initial burst release (6.45%). The microspheres prepared with CAB polymer showed faster dissolution rate than other polymers with 0.75: 1 drug to polymer ratio. The double emulsion technique with EC as wall material gave the high dissolution efficiency (80.48%) of microcapsules. Conclusions: Eudragit RS microspheres showed higher yield (90%). The release of TH from CAB and Eudragit RL walled microcapsules was slow whilst the release from those of EC and Eudragit RS were faster. The type of polymer and the drug to polymer ratio were found to be the key factors affecting the release profile which could lead to microspheres with desired release behavior.

A B S T R A C T Background:Microencapsulation is a useful method to prolong a drug release from dosage forms and to reduce its adverse effect (1) among various available methods. The microencapsulation of hydrophilic active ingredients requires the use of a polar dispersing phase such as a mineral oil. Acetone/paraffin systems are conventionally used. Objectives: The current study aimed to investigate two different microencapsulation techniques comparatively, water in oil in oil (w/o/o) and oil in oil (o/o), for theophylline (TH) loaded ethylcellulose (EC), cellulose acetate butyrate (CAB), Eudragit RS and RL microspheres with regard to loading efficiency, release and degradation kinetics. Materials and Methods: Microspheres were prepared by the emulsification method by solvent diffusion/evaporation technique and different polymers which were incorporated into microspheres to control the release rate of drug. Theophylline (TH) was chosen as a model drug. The emulsion technique was investigated for to prepare theophylline microparticles. EC and CAB and acrylatemethacrylate copolymer corresponding to the above ratios were selected as microparticles wall materials. The effects of type polymers on the physical characteristics and dissolution of the microparticles were also studied. However, the TH loading efficiency (for w/o/o emulsion about 90.64% and o/o emulsion about 73.90/5 to 95.90%) and the TH release kinetics were influenced by the microencapsulation technique. Results:The results demonstrated that the o/o microspheres (containing of CAB) was most appropriate, providing a high encapsulation efficiency (95.90%) and low initial burst release (6.45%). The microspheres prepared with CAB polymer showed faster dissolution rate than other polymers with 0.75: 1 drug to polymer ratio. The double emulsion technique with EC as wall material gave the high dissolution efficiency (80.48%) of microcapsules. Conclusions: Eudragit RS microspheres showed higher yield (90%). The release of TH from CAB and Eudragit RL walled microcapsules was slow whilst the release from those of EC and Eudragit RS were faster. The type of polymer and the drug to polymer ratio were found to be the key factors affecting the release profile which could lead to microspheres with desired release behavior.

Background: Targeted drug delivery to colon would ensure direct treatment at the disease site, decrease in dose administration and reduction side effects improved drug utilization. Objective: The purpose of this research was to decrease gastric side effects of piroxicam by formulating microspheres of alginate and algino-pectinate beads of the drug. Materials and Methods: Ionotropic gelation was used to entrap piroxicam into alginate and algino-pectinate mucoadhesive microspheres as a potential drug carrier for oral delivery of piroxicam. Microparticles with different drug to polymers ratio were prepared and characterized by encapsulation efficiency, particle size, DSC (differential scanning calorimetric), mucoadhesive property, gastroretentive time and drug release studies. Results:The best drug to polymer ratio of microparticles was 1:2.5 (F 1 ) with Na-Alg and 1:7.5 (F 4 ) with Alg-Na with pectin, respectively. The microparticles F 1 and F 4 showed 28.80%, 50.01% loading efficiency, 82.57%, 82.31% production yield and 945.4, 899.91 µm mean particle size. DSC showed stable character of piroxicam in drug-loaded microparticles and revealed amorphous form. It was found that microparticles (Na-Alg) prepared had faster release and microparticles (Alg-Na and pectin mixture) prepared had slower release than untreated piroxicam (P < 0.05). Microparticles (mixture of Na-Alg and pectin) exhibited very good percentage of mucoadhesion and flowability properties. Mucoadhesion strength and retention time study showed better retention of piroxicam microparticles in intestine. Besides, there was a significant higher retention of mucoadhesive microparticles in upper GI tract. Conclusions: Algino-pectinate mucoadhesive formulations exhibited promising properties of a sustained release form for piroxicam and provided distinct tissue protection in stomach. BackgroundIn general, rapid absorption from mucous routes is observed because of thin mucus membrane and rich blood supply. After absorption, drug is transferred by the deep lingual vein or facial vein and then drains into the general circulation via the jugular vein, bypassing the liver and thereby sparing the drug from first-pass metabolism. The term 'mucoadhesive' describes materials that bind to biological substrate, such as mucosal membranes. Adhesion of mucoadhesive drug delivery devices to mucosal membranes increases drug concentration gradient at the absorption site and therefore improves the bioavailability of systemically delivered drug (1). Polysaccharides polymers such as alginates have been investigated in the last years as carrier for controlled drug release (2, 3), cell encapsulation (4), tissue engineering material (5), or taste masking in pediatric formulations (6). Encapsulation property of alginate is due to its ability to move from sol to gel state by ionotropic gelation under mild conditions through interactions with bivalent or trivalent cations (7). The resulting particles are able to protect drugs from environmental stress or, based on alginate pH depend...