Preparation, Stabilization, and Dissolution Enhancement of Vortioxetine Hydrobromide Metastable Polymorphs in Silica Nanopores

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190422160115 ◽

2020 ◽

Vol 10 (5) ◽

pp. 649-663

Author(s):

Reena Siwach ◽

Parijat Pandey ◽

Harish Dureja

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Oral Absorption ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Class Ii ◽

Dissolution Enhancement ◽

In Vitro Drug Release ◽

Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

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Synthesis and Characterization of Nano-Sized 4-Aminosalicylic Acid–Sulfamethazine Cocrystals

Pharmaceutics ◽

10.3390/pharmaceutics13020277 ◽

2021 ◽

Vol 13 (2) ◽

pp. 277 ◽

Cited By ~ 1

Author(s):

Ala’ Salem ◽

Anna Takácsi-Nagy ◽

Sándor Nagy ◽

Alexandra Hagymási ◽

Fruzsina Gősi ◽

...

Keyword(s):

High Power ◽

Active Pharmaceutical Ingredient ◽

Polymorphic Form ◽

Degree Of Crystallinity ◽

Dissolution Enhancement ◽

Aminosalicylic Acid ◽

Nano Technology ◽

Power Ultrasound ◽

High Power Ultrasound ◽

High Degree

Drug–drug cocrystals are formulated to produce combined medication, not just to modulate active pharmaceutical ingredient (API) properties. Nano-crystals adjust the pharmacokinetic properties and enhance the dissolution of APIs. Nano-cocrystals seem to enhance API properties by combining the benefits of both technologies. Despite the promising opportunities of nano-sized cocrystals, the research at the interface of nano-technology and cocrystals has, however, been described to be in its infancy. In this study, high-pressure homogenization (HPH) and high-power ultrasound were used to prepare nano-sized cocrystals of 4-aminosalysilic acid and sulfamethazine in order to establish differences between the two methods in terms of cocrystal size, morphology, polymorphic form, and dissolution rate enhancement. It was found that both methods resulted in the formation of form I cocrystals with a high degree of crystallinity. HPH yielded nano-sized cocrystals, while those prepared by high-power ultrasound were in the micro-size range. Furthermore, HPH produced smaller-size cocrystals with a narrow size distribution when a higher pressure was used. Cocrystals appeared to be needle-like when prepared by HPH compared to those prepared by high-power ultrasound, which had a different morphology. The highest dissolution enhancement was observed in cocrystals prepared by HPH; however, both micro- and nano-sized cocrystals enhanced the dissolution of sulfamethazine.

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