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

(1 citation statement)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…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

View full text Add to dashboard Cite

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.

show abstract

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

View full text Add to dashboard Cite

show abstract

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

View full text Add to dashboard Cite

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.

show abstract

Construction of hyperbranched polysiloxane-based multifunctional fluorescent prodrug for preferential cellular uptake and dual-responsive drug release

Zhao

Liu²,

Lou

et al. 2022

Biomaterials Advances

View full text Add to dashboard Cite

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

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

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

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

Construction of hyperbranched polysiloxane-based multifunctional fluorescent prodrug for preferential cellular uptake and dual-responsive drug release

Contact Info

Product

Resources

About