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Development and evaluation of polymeric nanogels to enhance solubility of letrozole

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Abstract

This study scrutinized the use of monomer hydroxyethyl methacrylate, 2-carboxyethyl acrylate, initiator ammonium persulfate and cross-linker N′N′-methylene bisacrylamide to form polymeric composites by employing free radical polymerization of poorly water-soluble drug Letrozole (LTE). Letrozole is an aromatase inhibitor used in the treatment of breast cancer. Swelling index %, entrapment efficiency and solubility studies of developed formulations (LTE1-LTE9) were evaluated. Swelling studies indicated an increased swelling index at pH 7.4. The solubility of developed formulation was enhanced as compared to pure drug and β-cyclodextrin-Letrozole complex. Characterization of developed polymeric composites was performed by FTIR, DSC/TGA, SEM, XRD and zeta size. FTIR studies confirmed the encapsulation of Letrozole within polymeric composites. DSC/TGA indicated a thermally stable formulation. Surface morphology was assessed by SEM. XRD confirmed the amorphous formulation. The release study followed the Korsmeyer–Peppas model. In toxicity studies, clinical observations, hematological parameters and histopathological studies showed that developed polymeric composites were not toxic. Conclusively, our findings suggest that developed polymeric composites were safe and increased the solubility of poorly water-soluble drug and can be used as an effective platform for other hydrophobic drugs.

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Data availability

1. The authors confirm that the data supporting the findings of this study are available within the article. 2. Raw data were generated at Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad-Punjab, Pakistan. 3. The data that support the findings of this study are available on request from the corresponding author.

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Authors and Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Kotwali Road, Gurunanakpura, Faisalabad, 38000, Punjab, Pakistan

    Waqas Ahmad, Ikrima Khalid, Ikram Ullah Khan, Haroon Khaild Syed & Azka Ikram

  2. Department of Pharmaceutics, College of Pharmacy, University of Sargodha, Sargodha, Punjab, Pakistan

    Muhammad Usman Minhas

  3. Faculty of Pharmacy, The University of Lahore, Lahore, Punjab, Pakistan

    Kashif Barkat

  4. Department of Pharmacy, Capital University of Science and Technology, Islamabad, Pakistan

    Nadia Shamshad Mali

  5. Department of Pharmacy, The Islamia University of Bahawalpur-Punjab, Bahawalpur, Pakistan

    Ayesha Jamshed

  6. Islam College of Pharmacy, Sialkot, Punjab, Pakistan

    Munair Badshah

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  1. Waqas Ahmad
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  2. Ikrima Khalid
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  4. Muhammad Usman Minhas
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Correspondence to Ikrima Khalid.

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Ahmad, W., Khalid, I., Barkat, K. et al. Development and evaluation of polymeric nanogels to enhance solubility of letrozole. Polym. Bull. 80, 4085–4116 (2023). https://doi.org/10.1007/s00289-022-04248-5

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