Hydroxypropyl methylcellulose-based micro- and nanostructures for encapsulation of melanoidins: Effect of electrohydrodynamic processing variables on morphological and physicochemical properties

Author(s):  
P.M. Silva ◽  
C. Prieto ◽  
C.C.P. Andrade ◽  
J.M. Lagarón ◽  
L.M. Pastrana ◽  
...  
2021 ◽  
Vol 14 (5) ◽  
pp. 453
Author(s):  
Gabriela Wiergowska ◽  
Dominika Ludowicz ◽  
Kamil Wdowiak ◽  
Andrzej Miklaszewski ◽  
Kornelia Lewandowska ◽  
...  

To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect.


Author(s):  
TEJASWINI MANE ◽  
MUKESH MOHITE

Objective: Most of the drugs are relevant to BSC class II and class IV having solubility problems. Cocrystallization of drug with conformer is an immense approach used to explore the physicochemical properties of drug. The objective of the present work was to design formulate and evaluate the drug cocrystals of poorly soluble drug apremilast (APR) with saccharin. Methods: Cocrystals of APR were prepared using the solvent evaporation technique. The saturated solubility study and in vitro dissolution study of cocrystals were carried out. The prepared cocrystals were characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier-transform infrared (FTIR) spectroscopy. The topical gel of APR cocrystals was formulated optimized and evaluated using three-level factorial design. Results: The cocrystals of APR were prepared in 1:1 molar ratio with saccharin. APR cocrystals showed the improvement in solubility and dissolution as compared to pure APR. The formation of cocrystals was confirmed from change in endothermic peak of DSC and from shifting of FTIR spectra of cocrystals. Crystallinity of cocrystal was confirmed from XRD pattern and noteworthy change in 2θ values of the intense peak. The topical gel of APR cocrystals was formulated and optimized using three-level factorial design using Carbapol-940 and hydroxypropyl methylcellulose (HPMC) as a gelling agent. Conclusion: The cocrystals with altered physicochemical properties of APR were prepared with saccharin and formulated as a topical gel to overcome the problems related to oral administration.


Author(s):  
Majid Rajaee ◽  
Amir Talachi ◽  
Abbas Pardakhty ◽  
Ehsan Mohajeri ◽  
Negar Dehghannoudeh ◽  
...  

Background: Oral mucositis is a common debilitating complication of cancer chemotherapy and radiotherapy that can reduce the quality of patient’s lives. Hence, treating this condition plays an important role in increasing the patient’s tolerance. Objectives: Doxepin mucoadhesive gel is useful for treating oral mucosa inflammation caused by long-term effects of chemotherapy, which has low adverse effects. Methods: Doxepin gel’s formulation was prepared with various concentrations of poloxamer 407 and hydroxypropyl methylcellulose in deionized water. The prepared gels were evaluated for pH, appearance, viscosity, spreadability, stability, and drug release. Results: After providing gels containing doxepin, formulations 1, 2, 8, and 9 had low quality and, thus, were removed from the study. Based on qualitative evaluations, formulations 3 and 4 did not meet the criteria for mucoadhesive gel and were removed from the study. The best formulation contained 17% w/w poloxamer 407, 10% w/w hydroxypropyl methylcellulose, and 5% w/w doxepin. Conclusions: Suitable physicochemical properties of prepared doxepin mucoadhesive gel enable it to well cover inflamed and damaged oral mucosa. On the other hand, doxepin’s slow release from formulation (8 hours) can increase therapeutic effects and reduce side effects, which can heal and soothe inflammations of the oral mucosa and be useful in cancer patient’s treatment.


2015 ◽  
Vol 2015 ◽  
pp. 1-10 ◽  
Author(s):  
Ewa Brychcy ◽  
Dominika Kulig ◽  
Anna Zimoch-Korzycka ◽  
Krzysztof Marycz ◽  
Andrzej Jarmoluk

The treatment with acidic electrolyzed water (AEW) is a promising disinfection method due to its effectiveness in reducing microbial population. The aim of the study was to evaluate physicochemical properties of chitosan/HPMC films incorporated with lysozyme and acidic electrolyzed water. In the composite films, decreasing film solubility and increasing concentration of sodium chloride solution and prolongation of electrolysis time were observed. Electrolysis process with sodium chloride induces spongy network of film structure. The use of AEW has not changed chemical composition of films which was proved by1H NMR, MALDI-TOF, and FT-IR spectroscopy. The research confirmed that electrolysis significantly improved thermomechanical properties of the examined films. The contact angle values of the films were quite similar and ranged between 56° and 73°. The increase of salt concentration used in the electrolysis process had an impact on increasing flexibility of samples. Application of electrolyzed water in commonly used food processing systems is possible. Fusion of AEW and biopolymers may provide better integration with coated food product and multidirectional protecting effect.


2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Roya Yadollahi ◽  
Krasimir Vasilev ◽  
Clive A. Prestidge ◽  
Spomenka Simovic

The aim of the present research is to formulate and evaluate polymeric nanosuspensions containing three model water insoluble drugs, nifedipine (NIF), carbamazepine (CBZ), and ibuprofen (IBU) with various physicochemical properties. The nanosuspensions were prepared from hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP) by a cosolvent technique with polyethylene glycol (PEG-300) and water as the cosolvents. Physicochemical and morphological characteristics of the nanosuspensions (particle size, polydispersity index, and crystallinity) have been correlated with the drug release behaviour. The effects of polymer, drug ratio on the physical, morphological, and dissolution characteristics of the drugs are reported. Drug release is significantly enhanced from the nanosuspensions; for example, the maximum NIF, IBU, and CBZ concentrations after 8-hour dissolution are increased approximately 37, 2, and 1.2 times, respectively, in comparison with the pure powdered drugs. Based on this solubilization enhancement performance, the nanosuspensions have potential for increasing the orally dosed bioavailability of NIF, IBU, and CBZ.


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