Abstract
The main purpose of this study was to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of Olmesartan (OLM) for enhancement of its solubility and dissolution rate. In this study, liquid SNEDDS containing Olmesartan was formulated and further developed into a solid form by the spray drying technique using Aerosil 200 as a solid carrier. Based on the preliminary screening of different unloaded SNEDDS formulae, eight formulae of OLM loaded SNEEDS were prepared using Capryol 90, Cremophor RH40 and Transcutol HP as oil, surfactant and cosurfactant, respectively. Results showed that the mean droplet size of all reconstituted SNEDDS was found to be in the nanometric range (14.91–22.97 nm) with optimum PDI values (0.036–0.241). All formulae also showed rapid emulsification time (15.46 ± 1.34–24.17 ± 1.47 s), good optical clarity (98.33% ± 0.16%–99.87% ± 0.31%) and high drug loading efficiency (96.41% ± 1.20%–99.65% ± 1.11%). TEM analysis revealed the formation of spherical and homogeneous droplets with a size smaller than 50 nm. In vitro release of OLM from SNEDDS formulae showed that more than 90% of OLM released in approximately 90 min. Optimized SNEDDS formulae were selected to be developed into S-SNEDDS using the spray drying technique. The prepared S-SNEDDS formulae were evaluated for flow properties, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), reconstitution properties, drug content and in vitro dissolution study. It was found that S-SNEDDS formulae showed good flow properties and high drug content. Reconstitution properties of S-SNEDDS showed spontaneous self-nanoemulsification and no sign of phase separation. DSC thermograms revealed that OLM was in solubilized form and FTIR supported these findings. SEM photographs showed smooth uniform surface of S-SNEDDS with less aggregation. Results of the in vitro drug release showed that there was great enhancement in the dissolution rate of OLM. To clarify the possible improvement in pharmacokinetic behavior of OLM S-SNEDDS, plasma concentration-time curve profiles of OLM after the oral administration of optimized S-SNEDDS formula (F3) were compared to marketed product and pure drug in suspension. At all time points, it was observed that OLM plasma concentrations in rats treated with S-SNEDDS were significantly higher than those treated with the drug in suspension and marketed product.
Highlights
The oral delivery route is the most convenient and preferred route for drug administration to achieve desired therapeutic effects and the greatest degree of patient compliance, especially for chronic condition diseases [1]
Oils can solubilize the lipophilic drug in a specific amount so they are the main excipients because they can increase the fraction of lipophilic drug transported via the intestinal lymphatic system, thereby increasing absorption from the GIT
It was concluded that the prepared liquid self-nanoemulsifying drug delivery systems (SNEDDS) was thermodynamically stable with good self-emulsification efficiency and having globule size in the nanometric range which may be physiologically stable
Summary
The oral delivery route is the most convenient and preferred route for drug administration to achieve desired therapeutic effects and the greatest degree of patient compliance, especially for chronic condition diseases [1]. Despite some clinical oral formulations having been developed, the low oral bioavailability of most drugs is still a major hurdle leading to challenges for pharmaceutical manufacturers to design delivery systems that can provide improved pharmacokinetic profiles and therapeutic responses [3]. An ideal oral drug delivery system must protect the drug from the degradation in the gastrointestinal tract and deliver the bioactive compounds to the specific area where it is better absorbed. Considerable effort has been made in the improvement of oral drug delivery, drug stability in the GIT, increasing drug solubility and furthering the bioavailability [4]. A range of novel strategies are currently being developed for efficient delivery of poor water-soluble drugs
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