Development and evaluation of polymeric nanogels to enhance solubility of letrozole

Ahmad, Waqas; Khalid, Ikrima; Barkat, Kashif; Minhas, Muhammad Usman; Khan, Ikram Ullah; Syed, Haroon K.; Mali, Nadia Shamshad; Jamshed, Ayesha; Ikram, Azka; Badshah, Munair

doi:10.1007/s00289-022-04248-5

Cited by 8 publications

(7 citation statements)

References 54 publications

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“…The significantly improved solubility of TGR might be credited to the hydrophilicity, nanodimension, larger surface area, amorphous nature, porosity, efficient drug loading, and swellability of the synthesized nanogels and reduced crystallinity of TGR in nanogels, as also confirmed by XRD and DSC analyses. Our findings are in accordance with the outcomes of previous studies intended to improve the solubility of hydrophobic drugs by employing nanogels as drug delivery platforms. , …”

Section: Resultssupporting

confidence: 92%

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation

Saleem,

Khalid,

Hussain

et al. 2024

ACS Omega

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In this study, we synthesized PVA-g-poly(AMPS) nanogels with the aim of enhancing the solubility and dissolution of ticagrelor (TGR). Ticagrelor, a noncompetitive, reversible P2Y12 receptor antagonist, is prescribed to treat acute coronary syndrome. Ticagrelor has restricted oral bioavailability (≈36%) because of its poor solubility and permeability. The free radical polymerization methodology was employed to synthesize nanogels with varied concentrations of poly(vinyl alcohol) (polymer), 2-acrylamido-2-methylpropanesulfonic acid (monomer), and N,N-methylene bis(acrylamide) (crosslinker). The prepared nanogels were analyzed by swelling studies, % drug entrapment efficiency (DEE), solubility studies, in vitro drug release studies, zeta sizer, Fourier transform infrared (FTIR) spectroscopy, powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). The optimized formulation (PA5) revealed a particle size of 45.86 nm, with a polydispersity index (PDI) of 0.41 and a %DEE of 85.1%. FTIR spectroscopy, XRD, and SEM confirmed the formation of crosslinked nanogels with amorphous and porous structures, and TGA/DSC proved their thermal stability. In vitro dissolution studies showed 99.91% drug release, and the ticagrelor solubility from the synthesized formulations was significantly improved up to 8.2-fold. All formulations followed the Korsmeyer−Peppas model with the Fickian diffusion as the release mechanism. The toxicity studies carried out on rats and the MTT assay on the Caco-2 cell line validated the biocompatibility of the nanogel formulations. The outcomes of the current study led to the conclusion that the PVA-g-poly(AMPS) nanogels synthesized by us could be used as dedicated pharmaceutical delivery systems to achieve enhanced solubility and dissolution of ticagrelor.

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Section: Resultssupporting

confidence: 92%

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation

Saleem,

Khalid,

Hussain

et al. 2024

ACS Omega

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“…Due to the encapsulation of MAD by fabricated nanogels, the intensity of certain peaks of MAD, i.e., 1538 and 2970 cm –1 were decreased to 1520 and 2950 cm –1 bands of the formulated nanogels (Figure E), respectively. There was no interaction seen between the MAD and nanogel’s excipients …”

Section: Resultsmentioning

confidence: 99%

Formulation and In Vitro Assessment of Polymeric pH-Responsive Nanogels of Chitosan for Sustained Delivery of Madecassoside

Suhail,

Chiu,

Ullah

et al. 2024

ACS Omega

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Madecassoside, a triterpenoid saponin compound mainly isolated from the gotu kola herb (Centella asiatica), shows an extensive range of biological activities, including antiapoptotic, antioxidant, anti-inflammatory, moisturizing, neuroprotective, and wound healing effects. It has been highly used in the management of eczema, skin wounds, and other diseases. Due to poor oral bioavailability, membrane permeability, and intestinal absorption, the clinical application of the madecassoside is limited. Hence, a drug carrier system is needed that not only sustains the release of the madecassoside but also overcomes the drawbacks associated with its administration. Therefore, the authors prepared novel pH-responsive chitosan-based nanogels for the sustained release of madecassoside. Free radical polymerization technique was used for cross-linking of polymer chitosan and monomer methacrylic acid in the presence of cross-linker N′,N′-methylene bis(acrylamide). The decrease in polymer crystallinity after polymerization and development of nanogels was demonstrated by XRD and FTIR analysis. The effects of nanogel contents on polymer volume, sol–gel analysis, swelling, drug loading, and release were investigated. Results indicated that high swelling and maximum release of the drug occurred at pH 7.4 compared to pH 1.2 and 4.6, indicating the excellent pH-sensitive nature of the engineered nanogels. High swelling and drug release were perceived with the integration of a high quantity of chitosan, while a decline was observed with the high integration of N′,N′-methylene bis(acrylamide) and methacrylic acid contents. The same effects of nanogel contents were shown for drug loading too. Sol fraction was reduced, while gel fraction was enhanced by increasing the chitosan load, N′,N′-methylene bis(acrylamide), and methacrylic acid. The Korsmeyer–Peppas model of kinetics was trailed by all nanogel formulations with non-Fickian diffusion. The results demonstrated that prepared nanogels can be employed for sustained release of the madecassoside.

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“…However, in diffractogram of unloaded and Dexibuprofen loaded polymeric nanogels no sharp peaks were observed, indicating a successful grafting of AMPS on the agarose backbone, presenting the amorphous nature of prepared nanogels. 50…”

Section: Resultsmentioning

confidence: 99%

“…2,48,49 However, in diffractogram of unloaded and Dexibuprofen loaded polymeric nanogels no sharp peaks were observed, indicating a successful grafting of AMPS on the agarose backbone, presenting the amorphous nature of prepared nanogels. 50 Swelling studies. Swelling studies are an important part of investigating the waterabsorbing capacity which could be a good determinant for drug release from loaded nanogels when they are in contact with the biological fluid.…”

Section: Characterizationmentioning

confidence: 99%

Fabrication and evaluation of cross-linked nanogels of Dexibuprofen

Ikram,

Khalid,

Khan

et al. 2024

Journal of Bioactive and Compatible Polymers

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The objective of this study was to design and develop an Agarose-based polymeric nanogel network system for solubility enhancement of a lipophilic drug, Dexibuprofen. Polymeric nanogels were synthesized through free radical polymerization where Agarose was cross-linked with 2-Acrylamido-2-methylpropane sulfonic acid (AMPS) in the presence of ammonium persulfate (APS) as an initiator and N, N’-Methylenebisacrylamide (MBA) as crosslinking agent. The resulting polymeric nanogels underwent a comprehensive characterization process including Fourier transform infrared (FTIR), particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermal gravimetric analysis (TGA), powder X-ray diffraction (PXRD), and swelling studies to confirm the preparation of a stable polymeric nanogel system. FTIR spectral findings revealed that Agarose was chemically cross-linked with AMPS and confirmed the successful insertion of AMPS chains on the Agarose backbone. Particle size analysis revealed a diameter of 168 nm with a zeta potential of −9.91 mV, providing assurance of a stable polymeric nanogel system. SEM images depicted a highly porous surface. DSC and TGA results showed a more thermally stable network system than individual ingredients. Swelling studies revealed an increased swelling ratio of polymeric nanogels at phosphate buffer of pH 6.8 than acidic buffer of pH 1.2. Dexibuprofen was efficiently loaded into a polymeric nanogel system with a high entrapment efficiency of up to 80%. The solubility of the drug was enhanced when introduced to a polymeric nanogel formulation when compared to pure drug. The system reproducibility was evaluated through in vitro drug release and kinetic modeling of drug release. Toxicity studies confirmed the formulation’s effectiveness, showcasing the developed polymeric nanogels as a promising option for delivering lipophilic drugs, with outstanding physicochemical properties, improved solubility, and minimal oral toxicity.

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Development and evaluation of polymeric nanogels to enhance solubility of letrozole

Cited by 8 publications

References 54 publications

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation

Crosslinked PVA-g-poly(AMPS) Nanogels for Enhanced Solubility and Dissolution of Ticagrelor: Synthesis, Characterization, and Toxicity Evaluation

Formulation and In Vitro Assessment of Polymeric pH-Responsive Nanogels of Chitosan for Sustained Delivery of Madecassoside

Fabrication and evaluation of cross-linked nanogels of Dexibuprofen

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