Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems

Thenmozhi, Kathavarayan; Yoo, Young Je

doi:10.1080/03639045.2017.1321658

Cited by 41 publications

(41 citation statements)

References 46 publications

(24 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Efforts to improve the solubility and dissolution rates of piperine have been investigated, including the development of a solid dispersion system with several polymers and water-soluble carriers [20,21], the formation of inclusion complexes with cyclodextrin [22][23][24], and the reduction of the particle size to nanoscale [25][26][27]. Although these methods have improved the solubility of piperine, some problems remain.…”

Section: Introductionmentioning

confidence: 99%

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

et al. 2020

View full text Add to dashboard Cite

The objectives of this study were to prepare and characterize a novel piperine–succinic acid multicomponent crystal phase and to evaluate the improvement in the solubility and dissolution rate of piperine when prepared in the multicomponent crystal formation. The solid-state characterization of the novel multicomponent crystal was performed by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform-infrared (FT-IR) spectroscopy. Solubility and dissolution rate profiles were evaluated in distilled water. The physical stability was evaluated under high relative humidity (75% and 100% RH). The determination of the single crystal X-ray diffraction structure revealed that this novel multicomponent crystal was a cocrystalline phase of piperine–succinic acid (2:1 molar ratio). The differential scanning calorimetry thermogram of the cocrystal showed a single and sharp endothermic peak at 110.49 °C. The cocrystal resulted in greater solubility and a faster dissolution rate of piperine than intact piperine. This improvement was a result of the formation of a channel structure in the cocrystal. In addition, the cocrystal was stable under a humid condition.

show abstract

Section: Introductionmentioning

confidence: 99%

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Piperine, an alkaloid with poor water solubility, has been prepared into SDs with sorbitol, PEG and PVP by solvent evaporation method [ 36 ]. Piperine SDs with three different kinds of carriers all exhibited superior performance for enhancement of dissolution compared to physical mixtures and pure piperine.…”

Section: Solid Dispersion Techniquementioning

confidence: 99%

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

et al. 2018

View full text Add to dashboard Cite

Over the past decades, a large number of drugs as well as drug candidates with poor dissolution characteristics have been witnessed, which invokes great interest in enabling formulation of these active ingredients. Poorly water-soluble drugs, especially biopharmaceutical classification system (BCS) II ones, are preferably designed as oral dosage forms if the dissolution limit can be broken through. Minimizing a drug’s size is an effective means to increase its dissolution and hence the bioavailability, which can be achieved by specialized dispersion techniques. This article reviews the most commonly used dispersion techniques for pharmaceutical processing that can practically enhance the dissolution and bioavailability of poorly water-soluble drugs. Major interests focus on solid dispersion, lipid-based dispersion (nanoencapsulation), and liquisolid dispersion (drug solubilized in a non-volatile solvent and dispersed in suitable solid excipients for tableting or capsulizing), covering the formulation development, preparative technique and potential applications for oral drug delivery. Otherwise, some other techniques that can increase the dispersibility of a drug such as co-precipitation, concomitant crystallization and inclusion complexation are also discussed. Various dispersion techniques provide a productive platform for addressing the formulation challenge of poorly water-soluble drugs. Solid dispersion and liquisolid dispersion are most likely to be successful in developing oral dosage forms. Lipid-based dispersion represents a promising approach to surmounting the bioavailability of low-permeable drugs, though the technique needs to traverse the obstacle from liquid to solid transformation. Novel dispersion techniques are highly encouraged to develop for formulation of poorly water-soluble drugs.

show abstract

“…Its potential in increasing the solubilization of several poorly soluble bioactive compounds including vanillin, reserpine, sinapic acid and apigenin has been very well reported in the literature [ 24 , 25 , 26 , 27 ]. Some formulation technologies including solid dosage forms [ 28 , 29 ], emulsion/self-emulsifying formulations [ 30 , 31 , 32 ], nanomedicine-based drug delivery systems [ 33 , 34 , 35 , 36 ] and solid dispersion technology [ 37 ] have been studied in order to enhance solubility and bioactivity/bioavailability of PPN. The solubility of PPN in pure solvents including pure water, pure propylene glycol (PG), pure polyethylene glycol-400 (PEG-400) and pure THP at ambient temperature was reported elsewhere [ 1 , 30 , 31 ].…”

Section: Introductionmentioning

confidence: 99%

Solubility Data of the Bioactive Compound Piperine in (Transcutol + Water) Mixtures: Computational Modeling, Hansen Solubility Parameters and Mixing Thermodynamic Parameters

2020

View full text Add to dashboard Cite

The solubility values and thermodynamic parameters of a natural phytomedicine/nutrient piperine (PPN) in Transcutol-HP (THP) + water combinations were determined. The mole fraction solubilities (xe) of PPN in THP + water combinations were recorded at T = 298.2–318.2 K and p = 0.1 MPa by the shake flask method. Hansen solubility parameters (HSPs) of PPN, pure THP, pure water and THP + water mixtures free of PPN were also computed. The xe values of PPN were correlated well with “Apelblat, Van’t Hoff, Yalkowsky–Roseman, Jouyban–Acree and Jouyban–Acree–Van’t Hoff” models with root mean square deviations of < 2.0%. The maximum and minimum xe value of PPN was found in pure THP (9.10 × 10−2 at T = 318.2 K) and pure water (1.03 × 10−5 at T = 298.2 K), respectively. In addition, HSP of PPN was observed more closed with that of pure THP. The thermodynamic parameters of PPN were obtained using the activity coefficient model. The results showed an endothermic dissolution of PPN at m = 0.6–1.0 in comparison to other THP + water combinations studied. In addition, PPN dissolution was recorded as entropy-driven at m = 0.8–1.0 compared with other THP + water mixtures evaluated.

show abstract

Enhanced solubility of piperine using hydrophilic carrier-based potent solid dispersion systems

Abstract: Results suggest that the piperine solid dispersions prepared with improved in vitro release exhibit potential advantage in delivering poorly water-soluble piperine as an oral supplement.

Cited by 41 publications

References 46 publications

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

Improved Solubility and Dissolution Rates in Novel Multicomponent Crystals of Piperine with Succinic Acid

Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs

Solubility Data of the Bioactive Compound Piperine in (Transcutol + Water) Mixtures: Computational Modeling, Hansen Solubility Parameters and Mixing Thermodynamic Parameters

Contact Info

Product

Resources

About