Investigation of hyperbranched Poly(glycerol esteramide) as potential drug carrier in solid dispersion for solubility enhancement of lovastatin

Muniandy, Amala; Lee, Choy Sin; Lim, Wen Huei; Pichika, Mallikarjuna Rao

doi:10.1016/j.jddst.2020.102237

Cited by 6 publications

(5 citation statements)

References 35 publications

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“…This approach resulted in a substantial enhancement of the in vitro dissolution of lovastatin. Furthermore, this particular formulation achieved over a two-fold increase in cumulative drug release and a more than three-fold increase in solubility compared to pure lovastatin [29] .…”

Section: Solid Dispersionsmentioning

confidence: 95%

Exploration of Solubilization Strategies: Enhancing Bioavailability for Low Solubility Drugs

G. K.,

2023

ijnrph

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This review explores various strategies aimed at improving the solubilization of low-solubility drugs, including formulation design, nanoparticle technologies, prodrug strategies, and particle size reduction methods. Water solubility plays a crucial role in shaping bioavailability, formulation strategies, and therapeutic efficacy. Nanotechnology, particularly in nanomedicines, is a promising avenue to tackle solubility challenges, but faces barriers like production costs, formulation reproducibility, and varying pharmacokinetics. Despite these challenges, the burgeoning landscape of innovative drug delivery technologies offers advantages, particularly for formulation scientists. Understanding molecular properties is crucial for resolving these challenges, with solid dispersions and lipid-based delivery techniques emerging as sought-after solutions. Commercializing these advancements requires a leap in technology and infrastructure, making it essential to streamline the process and identify optimal approaches. Pioneering methodologies, such as Fagerholm's predictive model for human oral bioavailability based on chemical structure, demonstrate promising predictive accuracy. The integration of artificial intelligence and innovative solubility enhancement technologies is pivotal in transforming drug delivery, tackling solubility concerns, and streamlining research and development expenses.

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Section: Solid Dispersionsmentioning

confidence: 95%

Exploration of Solubilization Strategies: Enhancing Bioavailability for Low Solubility Drugs

G. K.,

2023

ijnrph

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“…Lovastatin stock solution of 20 μg mL −1 was prepared by sonicating 6 mg LOV in 300 mL of phosphate buffer saline (PBS) with 0.02% w/v sodium dodecyl sulfate (SDS) (pH 7.4) until a homogenous solution was obtained. LOV standard solutions of 18, 16, 14, 12, 10, 8, 6, 4, and 3.2 μg mL −1 were prepared by dilution from the stock solution 61 . The LOV standard solutions were quantified using a UV–Visible spectrophotometer (Shimadzu UV‐1800).…”

Section: Methodsmentioning

confidence: 99%

“…LOV standard solutions of 18, 16, 14, 12, 10, 8, 6, 4, and 3.2 μg mL À1 were prepared by dilution from the stock solution. 61 The LOV standard solutions were quantified using a UV-Visible spectrophotometer (Shimadzu UV-1800). Three sets of stock solution and standard solutions were prepared to obtain the average absorbances for the calibration curve (absorbances plotted against concentrations).…”

Section: Quantification Of Lovastatin Using Uv-vis Spectrophotometermentioning

confidence: 99%

“…The concentration of solution was estimated as an excess amount of 60 μg mL À1 . The samples were shaken at 150 rpm with a shaking incubator (Vision Scientific) at 37 ± 0.5 C for 24 h. 61 The samples were quantified with a UV-Vis spectrophotometer (Shimadzu UV-1800) at 239 nm and the absorbance was recorded. The experiment was conducted in triplicates and the average solubility was obtained.…”

Section: Solubility Study In Different Ph Mediummentioning

confidence: 99%

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pH‐responsive polyurethane‐acrylate from palm olein and sunflower oil: Sustainable synthesis, enhanced lovastatin solubility, and potential drug carrier for targeted delivery

Tan,

Lee,

Pichika

et al. 2024

J of Applied Polymer Sci

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A pH responsive non‐isocyanate polyurethane‐acrylate (NIPUA) is synthesized through utilizing palm olein and sunflower oil as feedstock. The unsaturated acyl chains of both vegetable oils are converted into epoxy rings through epoxidation and subjected to carbonation with binary catalytic system under a solventless and mild condition to produce the cyclic carbonates. The cyclic carbonates were reacted with 1,4‐butanediamine and itaconic acid to produce the NIPUA. The intermediates and product were characterized by FTIR spectroscopy, NMR spectroscopy and gel permeation chromatography. The NIPUA was incorporated with poly(vinyl pyrrolidone) (PVP) to form a polymer carrier system loaded with a hydrophobic model drug, lovastatin (LOV). All NIPUA/PVP preformulations demonstrated pH responsiveness, with 1 to 2‐folds enhanced solubility at pH 7.4 compared to pH 2.0. NIPUA/PVP exhibited solubility enhancer effect by significantly enhanced solubility (2–4 times) compared to pure LOV, LOV‐loaded PVP, and Medostatin tablets at both pH levels. LOV‐loaded NIPUA/PVP exhibited lower enthalpy energy in DSC thermogram than LOV‐loaded PVP, indicating disruption of LOV's crystalline structure. In MTT assay, IC50 values were 30.76 μg mL−1 for pure LOV and 273.53 μg mL−1 for NIPUA/PVP, demonstrating the potential of NIPUA as an environmentally friendly, pH responsive drug carrier for controlled release of poorly water‐soluble drugs.

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“…60% was used as a drug carrier in the fusion–solvent process to formulate lovastatin solid dispersions (LOV SD). SD having LOV:HPGEA = 5:95% w/w demonstrated significant improvement in in vitro dissolution, and the same formulation achieved a more than 2-fold increase in cumulative drug release and a more than 3-fold increase in solubility over pure LOV [ 50 ]. Various methods for preparing solid dispersions are discussed below:…”

Section: Conventional Approachesmentioning

confidence: 99%

Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs

Kumari

Choudhari

Patel

et al. 2023

Life

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A drug’s aqueous solubility is defined as the ability to dissolve in a particular solvent, and it is currently a major hurdle in bringing new drug molecules to the market. According to some estimates, up to 40% of commercialized products and 70–90% of drug candidates in the development stage are poorly soluble, which results in low bioavailability, diminished therapeutic effects, and dosage escalation. Because of this, solubility must be taken into consideration when developing and fabricating pharmaceutical products. To date, a number of approaches have been investigated to address the problem of poor solubility. This review article attempts to summarize several conventional methods utilized to increase the solubility of poorly soluble drugs. These methods include the principles of physical and chemical approaches such as particle size reduction, solid dispersion, supercritical fluid technology, cryogenic technology, inclusion complex formation techniques, and floating granules. It includes structural modification (i.e., prodrug, salt formation, co-crystallization, use of co-solvents, hydrotrophy, polymorphs, amorphous solid dispersions, and pH variation). Various nanotechnological approaches such as liposomes, nanoparticles, dendrimers, micelles, metal organic frameworks, nanogels, nanoemulsions, nanosuspension, carbon nanotubes, and so forth have also been widely investigated for solubility enhancement. All these approaches have brought forward the enhancement of the bioavailability of orally administered drugs by improving the solubility of poorly water-soluble drugs. However, the solubility issues have not been completely resolved, owing to several challenges associated with current approaches, such as reproducibility in large scale production. Considering that there is no universal approach for solving solubility issues, more research is needed to simplify the existing technologies, which could increase the number of commercially available products employing these techniques.

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Investigation of hyperbranched Poly(glycerol esteramide) as potential drug carrier in solid dispersion for solubility enhancement of lovastatin

Cited by 6 publications

References 35 publications

Exploration of Solubilization Strategies: Enhancing Bioavailability for Low Solubility Drugs

Exploration of Solubilization Strategies: Enhancing Bioavailability for Low Solubility Drugs

pH‐responsive polyurethane‐acrylate from palm olein and sunflower oil: Sustainable synthesis, enhanced lovastatin solubility, and potential drug carrier for targeted delivery

Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs

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