article · International Journal of Applied Pharmaceutics
Proniosomes were prepared to improve the dissolution characteristics of clopidogrel bisulphate. Using a slurry method with cholesterol, sorbitan monostearate, and maltodextrin as a carrier, various proniosomal formulations were created and tested. The resulting formulations achieved high drug entrapment efficiency between 83.04 percent and 90.14 percent. In laboratory release tests over four hours, the proniosomes released between 79.73 percent and 97.70 percent of the drug, significantly higher than the 61.77 percent release achieved by the plain drug. The optimal formulation was characterised for physical and chemical properties and tested in adult male mice. In these animal tests, the selected formulation significantly increased bleeding time and volume, prolonged prothrombin time, decreased prothrombin activity, and elevated the international normalised ratio compared to plain clopidogrel. Overall, the proniosome carrier system improved both the dissolution rate and the in vivo pharmacological activity of the medication.
Poor drug dissolution can limit how effectively medicines perform in the body. By using proniosomes as delivery carriers, this research demonstrates an effective way to improve the release rate of clopidogrel bisulphate. This enhancement translated into stronger antiplatelet action in animal models, showing how reformulation can potentially boost the therapeutic effectiveness of existing cardiovascular medications.
This work could enable pharmaceutical manufacturers to reformulate clopidogrel bisulphate into higher-performing oral dosage forms. The technology provides an improved delivery mechanism for cardiovascular therapies requiring reliable antiplatelet action. Because the research is applied and tested at the preclinical stage through laboratory dissolution and small-animal studies, it remains at an early development level and would require further formulation optimisation, safety evaluations, and clinical trials before commercial deployment.
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Objective: The present investigation aims to formulate and evaluate proniosomes of clopidogrel bisulphate for improving its dissolution characteristics.
 Methods: The slurry method was used for the preparation of proniosomes of clopidogrel using cholesterol, sorbitan monostearate (Span 60) and maltodextrin as a carrier. Clopidogrel proniosomes were evaluated for their entrapment efficiency and in vitro drug release. The best formula (F1) that achieved maximum drug release was further evaluated by measurement of the angle of repose, morphological examination, determination of vesicle size, determination of zeta potential, Fourier transform infrared spectroscopy and differential thermal analysis. The in vivo behavior of the selected proniosomal formula (F1) was studied by measuring the antiplatelet activity in adult male mice.
 Results: The entrapment efficiency of clopidogrel proniosomes was in the range of 83.04±1.99 to 90.14±0.30. % drug released from proniosomal formulations was in the range of 79.73±0.35 to 97.70±1.10 % within 4 h. Clopidogrel proniosomes significantly enhanced the in vitro release of clopidogrel compared with the plain drug that achieved 61.77±2.22 % drug release. F1 significantly (p ≤ 0.001) increased the bleeding time and bleeding volume and significantly (p ≤ 0.05) prolonged prothrombin time and decreased prothrombin activity and increased the international normalized ratio (INR) compared to plain clopidogrel.
 Conclusion: The present investigation introduced proniosomes as a promising carrier for clopidogrel that could enhance its dissolution and pharmacological effect.
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DOI: 10.22159/ijap.2019v11i2.30575
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