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<p>Solubility is one of the most important factors for therapeutic agents to show significant pharmacological response. Drugs that suffer from poor aqueous solubility are not absorbed in significant concentrations and hence their bioavailability is compromised and effectiveness of the drug is disrupted. In order to achieve the maximum absorption and significant bioavailability, solubility of the drug has to be enhanced. For this purpose, nanomatrices were formulated by free radical polymerization technique in order to enhance the solubility of acyclovir. The formulated nanomatrices were structurally characterized by Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD) and Particle Size Analysis. For in-vitro characterization, sol-gel fraction, swelling, in-vitro drug release and solubility studies of the formulated nanomatrices were carried out. Toxicity study was also performed in rabbits in order to access the biocompatibility of the formulated system with biological systems. According to FTIR spectroscopy, the unloaded and drug loaded nanomatrices were having specific functional groups of the individual components. According to SEM, the formulated nanomatrices were feasible for efficient loading of the drug while PXRD confirmed amorphous nature of the formulated nanomatrices. Average particle size of the formulated nanomatrices was 282.4 ± 09.43&#xa0;nm, confirming the nano-sized particles. According to swelling and drug release studies, it was observed that nanomatrices showed pH responsiveness and showed enhanced swelling and drug release in pH 6.8 as compared to pH 1.2. The optimized formulation showed a significant increase in the solubility of the drug as compared to the drug alone while toxicity study confirmed the biocompatibility of the system with the biological systems. Statistical analysis was also applied to determine the level of significance.</p>

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Characterization and safety evaluation of highly swellable polymeric nanomatrices for enhanced solubility of acyclovir

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年10月7日

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  • Ayesha Umar,
  • Kashif Barkat,
  • Syed Faisal Badshah,
  • Syed Nisar Hussain Shah,
  • Irfan Anjum,
  • Muhammad Umer Ashraf,
  • Muhammad Aamir,
  • Zulcaif,
  • Musaab Dauelbait,
  • Mohammad Khalid,
  • Amira Metouekel,
  • Abdullah R. Alanzi

摘要

Solubility is one of the most important factors for therapeutic agents to show significant pharmacological response. Drugs that suffer from poor aqueous solubility are not absorbed in significant concentrations and hence their bioavailability is compromised and effectiveness of the drug is disrupted. In order to achieve the maximum absorption and significant bioavailability, solubility of the drug has to be enhanced. For this purpose, nanomatrices were formulated by free radical polymerization technique in order to enhance the solubility of acyclovir. The formulated nanomatrices were structurally characterized by Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD) and Particle Size Analysis. For in-vitro characterization, sol-gel fraction, swelling, in-vitro drug release and solubility studies of the formulated nanomatrices were carried out. Toxicity study was also performed in rabbits in order to access the biocompatibility of the formulated system with biological systems. According to FTIR spectroscopy, the unloaded and drug loaded nanomatrices were having specific functional groups of the individual components. According to SEM, the formulated nanomatrices were feasible for efficient loading of the drug while PXRD confirmed amorphous nature of the formulated nanomatrices. Average particle size of the formulated nanomatrices was 282.4 ± 09.43 nm, confirming the nano-sized particles. According to swelling and drug release studies, it was observed that nanomatrices showed pH responsiveness and showed enhanced swelling and drug release in pH 6.8 as compared to pH 1.2. The optimized formulation showed a significant increase in the solubility of the drug as compared to the drug alone while toxicity study confirmed the biocompatibility of the system with the biological systems. Statistical analysis was also applied to determine the level of significance.