Effect of Nanotechnology Approaches on Anti-retroviral Molecule: Efavirenz

Krishnan, Priya Dharshini; Devi, D. Ramya; Hari, B.N. Vedha

doi:10.2174/1385272822666181116122616

Cited by 2 publications

(1 citation statement)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Improvements in the solubility of EFV have been reported in some studies through the preparation of co-crystals, the addition of superdisintegrant excipients, surfactants or cosolvency, amorphization, and the application of some technologies such as nanoemulsions, nanosuspensions, nanoparticles, and complex inclusion (10,(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30)(31). Some solid dispersion techniques are also used, including comminution to reduce particle size (22,(32)(33)(34)(35)(36)(37)(38).…”

Section: Introductionmentioning

confidence: 99%

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Wardhana¹,

Aisyah²,

Sopyan³

et al. 2021

Dissolution Technol.

View full text Add to dashboard Cite

Efavirenz (EFV) was approved by the United States Food and Drug Administration in 1998 with no polymorphic forms, but further research defined 23 different forms, including amorphous and solvated forms. This study aims to determine the ability of dissolved EFV polymorphs in in vitro media kinetic release models of pKa values. The polymorph types were obtained through various organic solvents such as acetonitrile, n-hexane, and methanol, i.e., form I, II, and III. The characteristics were distinguished by polarisation microscopy, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), and Raman spectroscopy. The solubility and dissolution of each polymorph were examined by adding 0.25% sodium lauryl sulphate (SLS) to the comparative dissolution media (water, HCl at pH 1.2, phosphate buffer at pH 4.6 and 6.8). The different microscopic shapes provided a unique fingerprint in the FTIR and the Raman spectra. The thermal behaviour examination provided a DSC thermogram with a specific melting point for each polymorph. The results of the solubility and dissolution tests reported that the highest peak was reached by form II, followed by forms III and I. These followed the pKa values of each polymorph, namely 10.12, 10.63, and 10.37 for form I, II, and III, respectively. The dissolution profile shows that pH conditions affect the release kinetics of form I compared to the metastable forms. The kinetic model of form I is pH-dependent; the acidic medium provided a slower release rate. Unlike the metastable forms, drug loading remained constant but still followed Higuchi's kinetic release model, even in acidic medium.

show abstract

Section: Introductionmentioning

confidence: 99%

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Wardhana¹,

Aisyah²,

Sopyan³

et al. 2021

Dissolution Technol.

View full text Add to dashboard Cite

show abstract

Current Progress in the Multicomponent Catalytic Synthesis of Amidoalkyl- Naphthols: An Update

Singh

Dhiman

Chaudhary

et al. 2020

COC

View full text Add to dashboard Cite

Amidoalkyl-2-naphthol is one of the vital synthetic intermediates which occupy an imperative position in medicinal chemistry due to its amazing biological, pharmacological as well as industrial and synthetic applications. Owing to its diverse pharmaceutical activities, hundreds of scientific literature are available, signifying the efficient synthesis of this intermediate using various catalysts. Most of these literature methods suffer from low yield and harsh reaction conditions that further ignited the researcher to explore for another green catalyst and fresh methodologies. This review summarizes the last five years progress in the catalytic synthesis of 1-amidoalkyl-2-naphthols using various heterogenous, homogenous and nanocatalysts along with their mechanism of action. Various advantages like green synthesis, atom economy, clean reaction profile and catalyst recovery are discussed which facilitate the scientist to probe and stimulate the study on this scaffold. In the end, the catalysts and reactions condition are organized into the tables for swift at a glance understanding of different catalysts used with their yield and time taken for the synthesis.

show abstract

Effect of Nanotechnology Approaches on Anti-retroviral Molecule: Efavirenz

Cited by 2 publications

References 0 publications

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

In Vitro Solubility and Release Profile Correlation with pKa Value of Efavirenz Polymorphs

Current Progress in the Multicomponent Catalytic Synthesis of Amidoalkyl- Naphthols: An Update

Contact Info

Product

Resources

About