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Preparation and evaluation of mucoadhesive beads/discs of alginate and algino-pectinate of piroxicam for colon-specific drug delivery via oral route.

Jelvehgari M, Mobaraki V, Montazam SH - Jundishapur J Nat Pharm Prod (2014)

Bottom Line: 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.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).Besides, there was a significant higher retention of mucoadhesive microparticles in upper GI tract.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, IR Iran ; Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, IR Iran.

ABSTRACT

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 (F1) with Na-Alg and 1:7.5 (F4) with Alg-Na with pectin, respectively. The microparticles F1 and F4 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.

No MeSH data available.


Histopathological Evaluation of Sections of Rat Abdominal MucosaA) Treated with microparticles discs (prepared with Na-Alg polymer); B), treated with microparticles discs (prepared with Na-Alg-Pectin) (magnitude X).
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fig13527: Histopathological Evaluation of Sections of Rat Abdominal MucosaA) Treated with microparticles discs (prepared with Na-Alg polymer); B), treated with microparticles discs (prepared with Na-Alg-Pectin) (magnitude X).

Mentions: The discs of all formulations had good appearance: 100.63-103.8% weight variation, 12.8-28 N hardness, and 0.84-9.05% friability (Table 3). The surface pH of all microparticles were in the range of 1.59-1.61 (pH = 1.2 in stomach) to 7.04-8.40 (pH = 6.8 in intestine). For discs F1 to F3 (prepared with Na-Alg polymer) and F4 to F8 (mixture of Na-Alg-Pectin polymers) ranged 1.060 to 1.271, which was in accordance with the referred value of 1.2 in stomach, but for discs F1 to F3 (7.37-7.89) and F4 to F8 (7.04-8.4) did not agree the referred value 6.8-7.4 in intestine (Table 5). Table 3 showed the percentage swelling of different microparticles formulations at different time intervals. It was revealed that all microsphere formulations swelled rapidly when immersed in 0.1 M phosphate buffer (pH = 6.8). In vitro residence time with rat abdominal mucosa in simulated gastric (pH = 1.2, 2 hours) and (pH = 6.8, 6 hours) varied for microparticles from 0 to 480 minutes (Table 3). Microparticles (F4 to F8) showed highest mucoadhesion in this study (180-480 minutes), and did not dissolve in 0.1 M HCl about 2 hours. For F1 formulation, time of microparticles remaining was 30-120 minutes. In contrast, microparticles containing mixture Na-Alg-Pectin polymers showed relatively higher retentive than formulations of prepared with single Na-Alg polymer. In vitro mucoadhesive strength study was performed and the results were shown in Table 3. On the modified physical balance and measure the force (g/cm2) required detaching the disc. The mucoadhesion characteristics were affected by the concentration of mucoadhesive polymers. The formulations (F1, F2 and F3) with Na-Alg showed the mucoadhesive strengths of 3.29, 4.81 and 6.56 g/cm2, respectively. Higher concentration of polymer (Na-Alg) increased mucoadhesive strength of formulation. F6 Formulation containing 1:12.5 ratio (drug: Na-Alg and Pectin) showed the highest mucoadhesion (11.14 ± 0.72 g/cm2). Microscopic observations revealed no significant effect of nanoparticles on the microscopic structure of mucosa. As shown in Figure 2, no cell necrosis was observed.


Preparation and evaluation of mucoadhesive beads/discs of alginate and algino-pectinate of piroxicam for colon-specific drug delivery via oral route.

Jelvehgari M, Mobaraki V, Montazam SH - Jundishapur J Nat Pharm Prod (2014)

Histopathological Evaluation of Sections of Rat Abdominal MucosaA) Treated with microparticles discs (prepared with Na-Alg polymer); B), treated with microparticles discs (prepared with Na-Alg-Pectin) (magnitude X).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4302400&req=5

fig13527: Histopathological Evaluation of Sections of Rat Abdominal MucosaA) Treated with microparticles discs (prepared with Na-Alg polymer); B), treated with microparticles discs (prepared with Na-Alg-Pectin) (magnitude X).
Mentions: The discs of all formulations had good appearance: 100.63-103.8% weight variation, 12.8-28 N hardness, and 0.84-9.05% friability (Table 3). The surface pH of all microparticles were in the range of 1.59-1.61 (pH = 1.2 in stomach) to 7.04-8.40 (pH = 6.8 in intestine). For discs F1 to F3 (prepared with Na-Alg polymer) and F4 to F8 (mixture of Na-Alg-Pectin polymers) ranged 1.060 to 1.271, which was in accordance with the referred value of 1.2 in stomach, but for discs F1 to F3 (7.37-7.89) and F4 to F8 (7.04-8.4) did not agree the referred value 6.8-7.4 in intestine (Table 5). Table 3 showed the percentage swelling of different microparticles formulations at different time intervals. It was revealed that all microsphere formulations swelled rapidly when immersed in 0.1 M phosphate buffer (pH = 6.8). In vitro residence time with rat abdominal mucosa in simulated gastric (pH = 1.2, 2 hours) and (pH = 6.8, 6 hours) varied for microparticles from 0 to 480 minutes (Table 3). Microparticles (F4 to F8) showed highest mucoadhesion in this study (180-480 minutes), and did not dissolve in 0.1 M HCl about 2 hours. For F1 formulation, time of microparticles remaining was 30-120 minutes. In contrast, microparticles containing mixture Na-Alg-Pectin polymers showed relatively higher retentive than formulations of prepared with single Na-Alg polymer. In vitro mucoadhesive strength study was performed and the results were shown in Table 3. On the modified physical balance and measure the force (g/cm2) required detaching the disc. The mucoadhesion characteristics were affected by the concentration of mucoadhesive polymers. The formulations (F1, F2 and F3) with Na-Alg showed the mucoadhesive strengths of 3.29, 4.81 and 6.56 g/cm2, respectively. Higher concentration of polymer (Na-Alg) increased mucoadhesive strength of formulation. F6 Formulation containing 1:12.5 ratio (drug: Na-Alg and Pectin) showed the highest mucoadhesion (11.14 ± 0.72 g/cm2). Microscopic observations revealed no significant effect of nanoparticles on the microscopic structure of mucosa. As shown in Figure 2, no cell necrosis was observed.

Bottom Line: 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.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).Besides, there was a significant higher retention of mucoadhesive microparticles in upper GI tract.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, IR Iran ; Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, IR Iran.

ABSTRACT

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 (F1) with Na-Alg and 1:7.5 (F4) with Alg-Na with pectin, respectively. The microparticles F1 and F4 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.

No MeSH data available.