Journal of Pharmaceutical Innovation最新文献

Purpose

This study was aimed to develop polymeric nanoparticles (PNPs) using chitosan (CTN), polyvinyl pyrrolidone (PVP), and Tween 80 for dissolution enhancement of poorly water-soluble antidiabetic drug: glimeperide (GLM).

Methods

GLM-loaded PNPs were developed for increasing the dissolution and solubility of GLM by using different amounts of CTN as polymer, PVP, and Tween 80 as stabilizers and tri-polyphosphate (TPP) as a crosslinking agent. PNPs were prepared using a combined approach of solvent evaporation and ionic gelation techniques. The newly fabricated PNPs were further characterized for percent encapsulation efficiency (%EE), compatibility studies, average particle size, morphology, thermal behavior, XRD examination, and dissolution studies at different biorelevant pH conditions.

Results

The prepared PNPs showed % encapsulation efficiency in the range of 55.90 to 93.25%. Fourier transform infrared studies revealed compatibility of GLM with formulation composites. The optimized PNPs F_1PVP and F_4TW80 showed particle size in nanoscale range 323 nm and 149 nm, respectively. SEM indicated formation of irregular (flakes) shaped particles. DSC and PXRD studies revealed reduction in crystallinity of the GLM inside PNPs thus promoting the dissolution. The dissolution studies at biorelevant acidic pH 1.2 and biorelevant basic pH 6.8 demonstrated remarkable improvement in dissolution profile compared to pure aqueous dispersion of GLM.

Conclusion

Overall results of the study suggested that CTN-based PNPs stabilized with PVP and Tween 80 can act as promising carriers for oral drug delivery of GLM.

Purpose

As Rosa damascena essential oils (RDEOs) have antioxidant, antibacterial, antiviral, and insecticidal activity, they could therefore be useful in the treatment of breast cancer. In the current study, an attempt was made to incorporate RDEO in a lipid-based drug delivery system, namely, nanostructured lipid carrier (NLC) to boost its anticancer effect compared to cisplatin.

Methods

Gas chromatography (GC) identified the chemical compositions of RDEO. RDEO-NLCs were prepared using the probe ultrasonication method. The obtained nanoparticles were characterized in terms of particle size, polydispersity index, and zeta potential by dynamic light scattering. The encapsulation efficiency of the formulations and their loading capacity were also determined, and transmission electron microscopy (TEM) was employed to evaluate the morphology of the optimal formulation (quoted as RDEO-NLC2). The anticancer effect of RDEO-NLC2 on MDA-MB-231 cells and apoptosis were assessed using MTT and in vitro cellular assays respectively.

Results

TEM result revealed a distinct spherical shape for RDEO-NLC2, with an average particle size of 78.39 ± 1.5 nm obtained by Zetasizer. The results also showed that the obtained particles had a negative surface charge (− 31.0 mV) with a polydispersity index of 0.28 ± 0.01. The chemotherapy drug cisplatin showed more cytotoxicity than RDEO-NLC2 against cancer cells. Cellular data demonstrated that RDEO-NLC2 like cisplatin can decline the viability of MDA-MB-231 cells through apoptosis compared to cells treated with the placebo and free RDEO.

Conclusion

RDEO-NLC2 has the ability to stimulate apoptosis in the human BC cell line MDA-MN-231; hence, it can be beneficial in the treatment of patients suffering from breast cancer.

Purpose

The study utilized non-ionic polymer macrogol to transform the surface properties of the DepoFoam drug carrier system, developing “surface-remodeled DepoFoam (SR-DFO)” following quality by design (QbD) principles. The primary objectives were to prolong drug delivery, reduce sudden releases, and enhance the overall quality and stability of DepoFoam. The research hypotheses are centered on the capability of macrogol-based surface modification to create an optimized drug delivery system with improved stability, extended drug release, and enhanced pharmacokinetic properties.

Methods

In this research, surface remodeling was achieved through a series of processes, including high-shear homogenizer-assisted double emulsification, PEGylation, and purification. The resulting SR-DFO formulations were comprehensively characterized for critical quality attributes. Optimization was conducted using the Box-Behnken design, resulting in significant enhancements in both quality and stability compared to conventional liposomes and unmodified DepoFoam.

Results

Comprehensive product characterization validates anticipated quality parameters: entrapment efficiency (86.16 ± 0.44%), drug-loading capacity (25.28 ± 0.07%), vesicle size (40.47 ± 0.1 µm), polydispersity index (PDI) of 0.051 ± 0.03, lipocrit of 90.67 ± 0.26%, and zeta potential of − 31.25 ± 3.25 mV. Remarkably, macrogol-based SR-DFO consistently sustains drug release above 90% for 168 h, devoid of sudden spikes, and maintains stability at 4 °C for 180 days. Mathematical models confirm drug release mechanisms’ validity. Moreover, this study emphasizes the critical influence of key materials like macrogol, phospholipids, triglycerides, and process variables on shaping product quality.

Conclusion

These findings highlight the inventive promise of macrogol-coated DFO in transforming drug delivery, quality, and stability. This research, driven by a well-formed hypothesis, meticulous execution, and precise data analysis, opens new horizons in polymer-based DepoFoam systems.

Graphical Abstract

First author: Jebastin Koilpillai, M.Pharm.

Purpose

The study aims to develop an interpenetrating polymer network (IPN) hydrogel bead. This drug carrier system with a hydrophilic polymer is designed through an ionotropic gelation technique using divalent calcium ions as a crosslinking agent. The resultant polymeric composite extends the release of the short-acting oral sulfonylurea drug, glipizide.

Methods

The IPN hydrogel beads prepared with more than one polymer bring forth better mechanical strength in contrast to a single polymeric-based network hydrogel system. This hydrogel bead of hydrophilic sodium alginate (SAL), the concentration of which ranges from 1.5 to 2.0% w/w, and xanthan gum (XAG) polymer, whose concentration ranges between 0.5 and 1.0% w/w, has been prepared to control the drug release profile. An ionotropic gelation technique with the crosslinking agent, calcium chloride at 2.5–7.5% w/w concentration, was adopted to prepare the IPN hydrogel bead drug carrier.

Results

The prepared hydrogel bead was studied for viscosity analysis of prepared composite dispersion, particle size, drug entrapment, swelling functions, and in vitro drug dissolution. An increase in xanthan gum quantity levels resulted in increased viscosity of prepared composite dispersions and hence the increased mean diameter of produced IPN hydrogel beads. Increased crosslinker concentration showed a slightly smaller IPN hydrogel bead mean diameter and increased encapsulation of loaded drug to about 88 to 91% glipizide. The in vitro drug dissolution was observed to be slower with increased xanthan gum polymer and calcium ion crosslinker concentration, which extended the drug release to 14 h. Thus, this work demonstrates that the XAG and calcium ion crosslinkers play a significant role in controlling the release of the loaded drug, glipizide.

Conclusion

Based on the results obtained, it can be concluded that the prepared novel polymeric-based IPN drug carrier system has beneficially controlled the drug release of short-acting oral sulphonyl medication and acted as an extended drug release system.

Purpose

This study aimed to prepare and characterize a topical niosomal formulation of benzoyl peroxide (BP) and clindamycin phosphate (CMP) for the treatment of acne vulgaris.

Methods

Different combinations of Polyoxyethylene Alkyl Ethers (Brij), sorbitan esters (Span), and their ethoxylated derivatives (Tween), and cholesterol were used to produce the niosomes. Encapsulation, release, chemical and physical stabilities of the prepared formulations were studied.

Results

The studied niosomes exhibited high physical stability, as evidenced by unchanged size distribution over a six-month storage period. Formulations composed of Brij-52 combined with 50 mol% of cholesterol showed the highest encapsulation efficiency for both CMP (81.5 ± 7.4%) and BP (95.6 ± 3.5%). The release rate of CMP was found to be greater than BP.

Conclusions

It was concluded that niosomes could serve as stable carriers for topical drug delivery of CMP and BP, specifically in the treatment of acne vulgaris.

Purpose

Monoclonal antibodies (mAbs) are important active ingredients of molecularly targeted drugs, which are only effective for specific patient groups. Early assessment of their effectiveness is important for more efficient use of time and resources. Companion diagnostics (CDx) are medical devices or tests to identify groups of promising patients based on specific biomarkers. This work offers a systems evaluation model and a comprehensive assessment from multiple stakeholder perspectives.

Methods

This work introduces a new systems model for assessing available treatment options. Process system diagrams, consisting of independently defined unit structures, are applied to represent the expected decision points and outcomes. A sensitivity analysis is conducted to identify the critical requirements for achieving cost-effectiveness. The model was applied to a case of terminal colorectal cancer treatment to compare mAb drugs to standard therapy.

Results

The results showed that from the payers’ perspective, the cost and response rates of the mAb drug were critical parameters to improve for achieving the target cost-effectiveness. The results give quantitative guidance for the required improvement.

Conclusion

This work represents an important step towards a fair and systematic assessment of treatment alternatives and serves as a guideline for future CDx and therapy technology development efforts.