Development And Evaluation Of Gastroretentive Microcapsules Of BCS Class II Drugs For Peptic Ulcer

4. Evaluation of Microcapsules

4.1 Percentage Yield

Percentage Yield=Practical YieldTheoretical Yield×100Percentage\ Yield = \frac{Practical\ Yield}{Theoretical\ Yield} \times 100Percentage Yield=Theoretical YieldPractical Yield​×100

4.2 Particle Size Analysis

Particle size was determined using optical microscopy.

4.3 Drug Entrapment Efficiency

Entrapment Efficiency (%)=Actual Drug ContentTheoretical Drug Content×100Entrapment\ Efficiency\ (\%) = \frac{Actual\ Drug\ Content}{Theoretical\ Drug\ Content} \times 100Entrapment Efficiency (%)=Theoretical Drug ContentActual Drug Content​×100

4.4 Micromeritic Properties

Bulk density, tapped density, Carr’s index, and angle of repose were evaluated.

4.5 Swelling Study

Swelling behavior was determined in simulated gastric fluid (pH 1.2).

Swelling Index=Wt−W0W0×100Swelling\ Index = \frac{W_t - W_0}{W_0} \times 100Swelling Index=W0​Wt​−W0​​×100

Where:

• WtW_tWt​ = Weight after swelling
• W0W_0W0​ = Initial weight

4.6 Buoyancy Study

Floating behavior was evaluated in simulated gastric fluid.

Floating Parameters

• Floating lag time
• Total floating duration

4.7 In Vitro Drug Release Study

Drug release study was carried out using USP dissolution apparatus II in 0.1 N HCl at 37 ± 0.5°C.

5. Fourier Transform Infrared Spectroscopy (FTIR)

FTIR studies were performed to determine drug-polymer compatibility.

6. Scanning Electron Microscopy (SEM)

Surface morphology of optimized microcapsules was examined using SEM.

7. Stability Studies

Accelerated stability studies were conducted at 40°C ± 2°C and 75% RH for three months according to ICH guidelines [8].

8. Statistical Analysis

Data were expressed as mean ± standard deviation. Statistical analysis was performed using one-way ANOVA.

RESULTS

1. Percentage Yield

Formulation F3 exhibited maximum percentage yield.

2. Particle Size Analysis

Particle size increased with increasing polymer concentration.

3. Drug Entrapment Efficiency

F3 showed highest drug entrapment efficiency.

4. Micromeritic Properties

The optimized formulation demonstrated good flow properties.

5. Swelling Study

The swelling index increased with time due to hydration of polymers.

6. Buoyancy Study

F3 exhibited excellent floating properties.

7. In Vitro Drug Release

The optimized microcapsules exhibited sustained drug release for 12 h.

8. FTIR Analysis

FTIR spectra showed no significant interaction between drug and polymers, confirming compatibility.

9. SEM Analysis

SEM images revealed spherical microcapsules with rough surface morphology and porous structure.

10. Stability Studies

The optimized formulation remained stable during accelerated storage conditions.

DISCUSSION

The present study successfully developed gastroretentive floating microcapsules of a BCS Class II antiulcer drug using ionotropic gelation technique.

Polymer concentration significantly influenced particle size, entrapment efficiency, swelling behavior, and drug release profile. Increased sodium alginate and HPMC concentrations improved entrapment efficiency due to formation of stronger polymeric matrices.

Floating microcapsules demonstrated prolonged buoyancy due to lower density and hydrated polymeric structure. Sustained drug release observed in optimized formulation may be attributed to controlled diffusion through swollen polymer matrix [9].

SEM studies confirmed formation of spherical porous microcapsules facilitating controlled release. Stability studies indicated good physicochemical stability under accelerated conditions.

The gastroretentive microcapsule system may improve therapeutic efficacy by maintaining prolonged gastric residence time and sustained drug release in the stomach.

CONCLUSION

The present investigation demonstrated successful development and evaluation of gastroretentive microcapsules for delivery of BCS Class II antiulcer drugs. The optimized formulation exhibited excellent floating behavior, sustained drug release, high entrapment efficiency, and good stability.

The developed gastroretentive system may enhance gastric retention, improve dissolution, and provide prolonged therapeutic action in peptic ulcer management. Further in vivo pharmacokinetic and clinical studies are necessary to establish therapeutic efficacy.

REFERENCES

1. Sung JJY, Kuipers EJ, El-Serag HB. Systematic review: The global incidence and prevalence of peptic ulcer disease. Aliment Pharmacol Ther. 2009;29(9):938–946.
2. Malfertheiner P, Chan FKL, McColl KEL. Peptic ulcer disease. Lancet. 2009;374(9699):1449–1461.
3. Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin Drug Deliv. 2006;3(2):217–233.
4. Rouge N, Allemann E, Gex-Fabry M, et al. Comparative pharmacokinetic study of gastroretentive systems. J Control Release. 1998;55(1):3–13.
5. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for BCS classification. Pharm Res. 1995;12(3):413–420.
6. Jain SK, Agrawal GP, Jain NK. Evaluation of porous carrier-based floating drug delivery system. AAPS PharmSciTech. 2006;7(4):E90.
7. Anal AK, Stevens WF. Chitosan–alginate multilayer beads. Int J Pharm. 2005;290(1-2):45–54.
8. ICH Q1A(R2). Stability Testing of New Drug Substances and Products. International Council for Harmonisation; 2003.
9. Singh BN, Kim KH. Floating drug delivery systems. J Control Release. 2000;63(3):235–259.
10. Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of novel controlled-release systems. Pharm Res. 1997;14(6):815–819.