Phospholipid-containing films for improved drug release

Phospholipids from natural sources can delay liquid-liquid phase separation and improve supersaturation for active pharmaceutical ingredients with poor water-solubility in aqueous media. Researchers have developed oral films containing phospholipids to enhance the dissolution efficiency of hydrophobic pharmaceutical ingredients. Phospholipid-based oral films provide an alternative approach for compounding pharmacies to formulate drugs with poor water solubility.

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems.

A multi-responsive self-healing hydrogel for control-release of curcumin

Curcumin is a traditional herbal medicine with immense therapeutic potential; however, its application is severely limited owing to its poor water solubility. In this study, a multi-responsive self-healing hydrogel for...

Hyperbranched polysiloxane containing carbon dots with near white light emission

Hyperbranched polysiloxane (HBPSi) has received widespread attention as an emerging non-traditional fluorescence polymer. However, it remains some drawbacks such as inadequate emission intensity and poor water solubility, which limit its...

Mechanism of enhancing the water-solubility and stability of curcumin by self-assembled cod protein nanoparticles at alkaline pH

Curcumin (Cur) is a bioactive phytochemical claimed to have several health-promoting benefits, whose applications are challenged due to its poor water-solubility, chemical instability, and low bioavailability. In this research, the...

Developments in Carbohydrate-Based Metzincin Inhibitors

Matrix metalloproteinases (MMPs) and A disintegrin and Metalloproteinase (ADAMs) are zinc-dependent endopeptidases belonging to the metzincin superfamily. Upregulation of metzincin activity is a major feature in many serious pathologies such as cancer, inflammations, and infections. In the last decades, many classes of small molecules have been developed directed to inhibit these enzymes. The principal shortcomings that have hindered clinical development of metzincin inhibitors are low selectivity for the target enzyme, poor water solubility, and long-term toxicity. Over the last 15 years, a novel approach to improve solubility and bioavailability of metzincin inhibitors has been the synthesis of carbohydrate-based compounds. This strategy consists of linking a hydrophilic sugar moiety to an aromatic lipophilic scaffold. This review aims to describe the development of sugar-based and azasugar-based derivatives as metzincin inhibitors and their activity in several pathological models.

Dissolution Enhancement of Eplerenone Using Solvent Melt Method

Background: Eplerenone (EPL) is a BCS class II drug, thus, having the poor water solubility. The poor water solubility of this drug leads to the poor dissolution and ultimately shows the poor bioavailability. To overcome this problem, the solid dispersion of EPL was prepared in this study. Methods: This was accomplished by using the solvent melt method as the solid dispersion technique. In this method Pluronic F-68 and F-127 was used as the carrier and different formulations were prepared using the varying in ratio of a drug and carrier (1:1, 1:2, 1:3, 1:4, 1:5). The mixture of drug solution and carrier were prepared at 70oC, using the digital magnetic stirrer. The resultant mixture was dried at 40oC in hot air oven and optimized EPL-solid dispersion was undergone for their characterization using drug content, drug entrapment efficiency (%) and drug loading content (%), Scanning Electron Microscopy (SEM), Infra-Red spectroscopy, Differential Scanning Calorimetery (DSC), stability study and in-vitro dissolution studies. Results: The result indicated that there was no interaction between EPL and Pluronics (Pluronic F-68 & F-127), and optimized formulation (P127-2) of EPL-solid dispersion have encapsulation efficiency > 95%. Experimental work also showed that optimized formulation has 31.7% of drug loading content which was greater than other existing solid dispersion having less than 30% of drug loading content. Out of different batches, the optimized batch exhibits the faster dissolution rate in comparison of other batches. It released the almost total amount of drug (98.96%) in 30 minutes. The stored ESM-solid dispersion also exhibited their remarkable stability and remains in solid state, when it was exposed to 25oC/60% relative humidity and room temperature (38ºC) for two months. Such stability was confirmed by DSC method. The DSC thermogram of optimized formulation exhibited a melting endotherm at onset temperature of 160oC, a peak temperature of 165oC and a heat of fusion of 25.68 J/gm. Simirly, DSC thermogram of physical mixture of bulk EPL/pluronic F-127 also exhibited the onset of temperature at 165oC, and a peak temperature at 171oC. Thus, result indicated that both sample showed the almost similar DSC pattern and no one sample alter their state after the treatment of temperature and humidity used in stability testing. SEM study was also performed in this research and result indicated that the particle size of optimized formulation was varied and having the irregular matrices due to porous nature of the carrier. Conclusion: Based on different findings it can be concluded that solvent melt method could be a potential method for preparing the solid dispersion of EPL like BCS class-II Drugs and will be able to solve the dissolution and solubilization related problem of poorly soluble drugs.

Pharmacokinetic Comparisons of Naringenin and Naringenin-Nicotinamide Cocrystal in Rats by LC-MS/MS

Naringenin (NAR), 4′,5,7-trihydroxydihydroflavone, has a wide range of pharmacological activities but shows poor water solubility and low bioavailability. The pharmacokinetics and bioavailability of naringenin-nicotinamide cocrystal (NAR-NCT), which offers improved solubility, were evaluated in this study. Rats were orally administered NAR, a physical mixture of naringenin and nicotinamide (NAR + NCT), and NAR-NCT. The relative bioavailability of NAR-NCT was 175.09% of NAR, Cmax was 8.43 and 2.06 times of NAR and NAR + NCT, respectively, Tmax was advanced from 0.49 h to 0.09 h, CL was decreased from 91.1 L/h/kg to 49.1 L/h/kg, and t1/2 was increased from 5.37 h to 8.24 h, highlighting its rapid absorption and slow elimination. This study showed that NAR-NCT could improve the bioavailability of NAR.

Transdermal delivery of rapamycin with poor water-solubility by dissolving polymeric microneedles for anti-angiogenesis

Rapamycin-loaded dissolving microneedles (RAPA DMNs) are fabricated by using polyvinylpyrrolidone (PVP) as the matrix and exhibit the good anti-angiogenic effect.