Mixed Avanafil and Dapoxetin Hydrochloride cyclodextrin nano-sponges: Preparation, in-vitro characterization, and bioavailability determination was written by Gardouh, Ahmed R.;Elhusseiny, Sameh;Gad, Shadeed. And the article was included in Journal of Drug Delivery Science and Technology in 2022.Formula: C13H10O3 The following contents are mentioned in the article:
Avanafil (AVA) and Dapoxetine hydrochloride are BCS Class II drugs, which means that the bioavailability depends on its solubility extent. Nano-sponges are hyper-crosslinked cyclodextrin nano-polymers that have been developed recently to make solid particles with nonporous structure; they’re prepared by reacting different types of cyclodextrins with an appropriate crosslinking agent like di-Ph carbonate. Nano-sponges can improve the solubility of poorly soluble active mols. and increase stability by protecting labile groups. Hence, the purpose of this work was to study the effects of different types of cyclodextrins and crosslinker ratios on the solubility and oral bioavailability of Avanafil (AVA) and Dapoxetine hydrochloride (DA) by loading them to Nano-sponges prepared by crosslinking of 尾-CD, SBE-尾-CD with di-Ph carbonate (DPC) as a crosslinker at various molar ratios. AVA and DA-loaded nano-sponges were fabricated using the freeze-drying method and characterized for particle size, zeta potential, loading capacities, and in-vitro drug release. SEM, differential scanning calorimetry, and Fourier transform IR spectroscopy were used to characterize the NS and AVA/DA incorporation within the NS. In-vitro drug release was significantly higher with AVA and DA-loaded nano-sponges. Furthermore, the results revealed that AVA and DA-loaded nano-sponges fabricated with 尾-CD had a higher release in dissolution with both drugs than those fabricated using SBE-尾-CD. AVA and DA-loaded nano-sponges increased the oral bioavailability of both drugs by 2.5 and 7.5 folds, resp., when compared to Spedra and Priligy. While there is no significant difference in Tmax between F10 and Spedra, E12 has a faster onset than Priligy. A one-way ANOVA revealed a substantial increase in Cmax and T1/2 for AVA and DA. Therefore, AVA and DA-loaded nano-sponges are considered a better alternate to the regular dosage forms for efficient AVA and DA oral delivery. This study involved multiple reactions and reactants, such as Diphenyl carbonate (cas: 102-09-0Formula: C13H10O3).
Diphenyl carbonate (cas: 102-09-0) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 纬-valerolactone.Formula: C13H10O3
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics