Abstract
Objective: The purpose of this study was to formulate and optimize mucoadhesive microspheres of antihypertensive drug (valsartan) within ethyl cellulose as a carrier polymer and carbopol 934P as a mucoadhesive polymer for controlling the release of valsartan.
 Methods: The emulsion solvent evaporation technique was used for preparation of microspheres of valsartan and the Box-Behnken design was employed with thee independent variables that is amount of ethyl cellulose (X1) and amount of carbopol 934P (X2) and stirring speed (X3) and evaluate four dependent variables such as percentage mucoadhesion, Q1 h, t90% and drug entrapment efficiency.
 Results: The optimum conditions were found to be X1= 200 mg, X2= 107 mg and X3= 1200rpm. The optimized batch exhibited a high drug entrapment efficiency of 85.63±1.384%, percentage mucoadhesion was 66.76±0.986% and drug release was also sustained for more than 12 h.
 Conclusion: The analysis of variance showed a significant effect of independent variables. The scaning electron microscopy (SEM) analysis showed that the microspheres were spherical and free-flowing. The microspheres of valsartan were stable after thee month stability study at accelerated condition.
Highlights
Hypertension is one of the primary risk factors for heart disease and stroke, the leading causes of death due to its high prevalence all around the globe [1,2,3,4]
In the Box-Behnken design, a total 15 formulations were proposed by Design expert software for thee factors such as the amount of ethyl cellulose (X1), amount of carbopol 934P (X2) and stirring speed (X3), which were varied at thee different levels (−1, 0 and 1)
The entrapment efficiency, Q1h, t90% and percent Mucoadhesion, analyzed though Box-Behnken design significantly affected by independent variables such as the amount of ethyl cellulose (X1), amount of carbopol 934P (X2) and stirring speed (X3)
Summary
Hypertension is one of the primary risk factors for heart disease and stroke, the leading causes of death due to its high prevalence all around the globe [1,2,3,4]. 7.5 million deaths worldwide occur due to hypertension and predicted to be increased to 1.56 billion adults with high blood pressure in 2025 [5, 6]. A number of different types of anti-hypertensive agents used to control elevated blood pressure [7]. A non-peptide, specific competitive angiotensin II type 1 receptor antagonist is a drug of choice in cardiovascular disorders, in hypertension [8, 9]. The oral route is most convenient for the delivery of different dosage form as compared with other routes [10]. Improving its therapeutic efficacy through oral route alternative drug delivery systems and dosage forms is needed [11,12,13]
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