scholarly journals Deaggregation and Crystallization Inhibition by Small Amount of Polymer Addition for a Co-Amorphous Curcumin-Magnolol System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1725
Author(s):  
Jiawei Han ◽  
Luyuan Li ◽  
Meiling Su ◽  
Weili Heng ◽  
Yuanfeng Wei ◽  
...  
Keyword(s):  
Physical Stability ◽  
Drug Dissolution ◽  
Amorphous Systems ◽  
Polymer Addition ◽  
Promising Strategy ◽  
Crystallization Inhibition ◽  
Water Wettability ◽  
Long Time ◽  
Enhanced Surface ◽  
Pvp K30

Different from previously reported co-amorphous systems, a co-amorphous curcumin-magnolol (CUR-MAG CM) system, as compared with its crystalline counterparts, exhibited decreased dissolution due to its aggregation during dissolution. The main purpose of the present study is to deaggregate CUR-MAG CM to optimize drug dissolution and explore the deaggregation mechanism involved. Herein, a small amount of polymer (HPMC, HPC, and PVP K30) was co-formulated at 5% (w/w) with CUR-MAG CM as ternary co-amorphous systems. The polymer addition changed the surface properties of CUR-MAG CM including improved water wettability enhanced surface free energy, and hence exerted a deaggregating effect. As a result, the ternary co-amorphous systems showed faster and higher dissolution as compared with crystalline CUR/MAG and CUR-MAG CM. In addition, the nucleation and crystal growth of dissolved CUR and MAG molecules were significantly inhibited by the added polymer, maintaining a supersaturated concentration for a long time. Furthermore, polymer addition increased the Tg of CUR-MAG CM, potentially involving molecular interactions and inhibiting molecular mobility, resulting in enhanced physical stability under 25 °C/60% RH and 40 °C/75% RH conditions. Therefore, this study provides a promising strategy to optimize the dissolution and physical stability of co-amorphous systems by deaggregation and crystallization inhibition via adding small amounts of polymers.

scholarly journals Electrospun Borneol-PVP Nanocomposites

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Xiao-Yan Li ◽  
Xia Wang ◽  
Deng-Guang Yu ◽  
Shuai Ye ◽  
Qi-Kun Kuang ◽  
...  
Keyword(s):  
High Performance ◽  
Drug Delivery Systems ◽  
Composite Nanofibers ◽  
Physical Stability ◽  
Electrospinning Process ◽  
Drug Dissolution ◽  
Uniform Structure ◽  
Hydrogen Bonding Interactions ◽  
Nano Drug Delivery ◽  
Long Time

The present work investigates the validity of electrospun borneol-polyvinylpyrrolidone (PVP) nanocomposites in enhancing drug dissolution rates and improving drug physical stability. Based on hydrogen bonding interactions andviaan electrospinning process, borneol and PVP can form stable nanofiber-based composites. FESEM observations demonstrate that composite nanofibers with uniform structure could be generated with a high content of borneol up to 33.3% (w/w). Borneol is well distributed in the PVP matrix molecularly to form the amorphous composites, as verified by DSC and XRD results. The composites can both enhance the dissolution profiles of borneol and increase its physical stability against sublimation for long-time storage by immobilization of borneol molecules with PVP. The incorporation of borneol in the PVP matrix weakens the tensile properties of nanofibers, and the mechanism is discussed. Electrospun nanocomposites can be alternative candidates for developing novel nano-drug delivery systems with high performance.

scholarly journals Development and Stability Studies of Novel Liposomal Vancomycin Formulations

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Krishna Muppidi ◽  
Andrew S. Pumerantz ◽  
Jeffrey Wang ◽  
Guru Betageri
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Antimicrobial Agents ◽  
Preparation Method ◽  
Physical Stability ◽  
Liposomal Formulations ◽  
Promising Strategy ◽  
Activity Variable ◽  
Distribution Studies

A promising strategy to improve the therapeutic efficiency of antimicrobial agents is targeted therapy. Although vancomycin has been considered a gold standard for the therapy of MRSA pneumonia, clinical failure rates have also been reported owing to its slow, time-dependent bactericidal activity, variable lung tissue penetration and poor intracellular penetration into macrophages. Liposomal encapsulation has been established as an alternative for antimicrobial delivery to infected tissue macrophages and offers enhanced pharmacodynamics, pharmacokinetics and decreased toxicity compared to standard preparations. The aim of the present work is to prepare vancomycin in two different liposomal formulations, conventional and PEGylated liposomes using different methods. The prepared formulations were optimized for their particle size, encapsulation efficiency and physical stability. The dehydration-rehydration was found to be the best preparation method. Both the conventional and PEGylated liposomal formulations were successfully formulated with a narrow particle size and size distribution and % encapsulation efficiency of and , respectively. Both the formulations were stable at C for 3 months. These formulations were successfully used to evaluate for their intracellular killing of MRSA and in vivo pharmacokinetic and bio-distribution studies.

scholarly journals Investigation Utilizing the HLB Concept for the Development of Moisturizing Cream and Lotion: In-Vitro Characterization and Stability Evaluation

Cosmetics ◽  
2020 ◽  
Vol 7 (2) ◽  
pp. 43 ◽  
Author(s):  
Shoaib Alam ◽  
Mohammed S. Algahtani ◽  
Mohammad Zaki Ahmad ◽  
Javed Ahmad
Keyword(s):  
Physical Stability ◽  
Storage Conditions ◽  
Phase System ◽  
Stability Evaluation ◽  
Stable Emulsion ◽  
Promising Strategy ◽  
In Vitro Characterization ◽  
Hydrophilic Lipophilic Balance ◽  
Droplet Morphology

The current study aims to utilize the concept of the hydrophilic–lipophilic balance (HLB) value of ingredients for the development of a stable emulsion-based moisturizing cream and lotion for cosmetic application. The combination of a hydrophilic and lipophilic emulsifier such as glyceryl stearate (HLB value 3.8) and PEG-100 stearate (HLB value 18.8) were found to be effective to emulsify the chosen oil phase system at a specific concentration to achieve the required HLB for the development of the stable emulsion-based system. The developed formulation was characterized for pH, viscosity, spreadability, rheology, and droplet morphology. The influence of carbopol® ETD 2020 and the concentration of the oil phase on the rheology of the product was investigated and found to be significant to achieve the required thickening to convert the lotion into a cream. The formulation system developed through utilizing the concept of HLB was compared to a product developed through the conventional approach. It was observed that the utilization of the HLB method for the development of an emulsion-based product is a promising strategy compared to the conventional method. The physical stability and thermodynamic stability tests were carried out under different storage conditions. It was observed that the developed formulation was able to retain its integrity without showing any signs of instability during storage.

IMPROVEMENT OF DISSOLUTION RATE OF FEBUXOSTAT USING HYBRID TECHNIQUE OF SPHERICAL CRYSTALLIZATION AND SOLID DISPERSION

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 32-39
Author(s):  
D. B Tandel ◽  
◽  
P. A Shah ◽  
K. G. Patel ◽  
M. C Gohel ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Hybrid Technique ◽  
Spherical Crystallization ◽  
Spherical Agglomerates ◽  
Pvp K30 ◽  
Excipient Compatibility

The present study was carried out with an aim to improve dissolution rate of febuxostat (FBX, BCSclass II) drug. Spherical agglomerates were prepared by hybrid technique of spherical crystallization and solid dispersion using different ratios of FBX and polymer (PVP K30, HPMC E3LV and chitosan). Drug excipient compatibility study was evaluated by Fourier transform infrared spectroscopy and X-ray diffractometry. Scanning electron microscopy was used for measurement of size of agglomerate. In vitro dissolution study of prepared spherical agglomerates was compared with untreated FBX and marketed formulation in phosphate buffer pH 6.8. The ratio of drug to polymer also affected the drug dissolution results. Drug excipient compatibility study showed no interaction between FBX and PVP K30 (1:5) polymer. The use of PVP K30 (1:5) resulted in partial amorphization and improved drug dissolution. Direct compression method can be adopted in manufacturing to simplify the validation efforts. The performance of the formulated product was superior to the marketed product in the in vitro dissolution test.

Transformations between Co-Amorphous and Co-Crystal Systems and Their Influence on the Formation and Physical Stability of Co-Amorphous Systems

2019 ◽  
Vol 16 (3) ◽  
pp. 1294-1304 ◽  
Author(s):  
Wenqi Wu ◽  
Yixuan Wang ◽  
Korbinian Löbmann ◽  
Holger Grohganz ◽  
Thomas Rades
Keyword(s):  
Physical Stability ◽  
Amorphous Systems

scholarly journals A Multivariate Approach for the Determination of the Optimal Mixing Ratio of the Non-Strong Interacting Co-Amorphous System Carvedilol-Tryptophan

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 801
Author(s):  
Rong Di ◽  
Jingwen Liu ◽  
Holger Grohganz ◽  
Thomas Rades
Keyword(s):  
Physical Stability ◽  
Principal Component ◽  
Water Soluble ◽  
Mixing Ratio ◽  
Scanning Calorimetry ◽  
Amorphous Systems ◽  
Amorphous System ◽  
Novel Approach ◽  
Water Soluble Drugs ◽  
Optimal Mixing

Converting crystalline compounds into co-amorphous systems is an effective way to improve the solubility of poorly water-soluble drugs. It is, however, of critical importance for the physical stability of co-amorphous systems to find the optimal mixing ratio of the drug with the co-former. In this study, a novel approach for this challenge is presented, exemplified with the co-amorphous system carvedilol–tryptophan (CAR–TRP). Following X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) of the ball-milled samples to confirm their amorphous form, Fourier-transform infrared spectroscopy (FTIR) and principal component analysis (PCA) were applied to investigate intermolecular interactions. A clear deviation from a purely additive spectrum of CAR and TRP was visualized in the PCA score plot, with a maximum at around 30% drug (mol/mol). This deviation was attributed to hydrogen bonds of CAR with TRP ether groups. The sample containing 30% drug (mol/mol) was also the most stable sample during a stability test. Using the combination of FTIR with PCA is an effective approach to investigate the optimal mixing ratio of non-strong interacting co-amorphous systems.

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