Quality by design enabled self-nano emulsifying drug delivery systems development for the oral delivery of telmisartan: Improvement of biopharmaceutical performance

Abstract

Purpose: To increase the drug's oral bioavailability, a self-nano emulsifying drug delivery system was designed using capmul MCM, labrasol, and tween-20 as the oil, surfactant, and co-surfactant, respectively. Oil and Smix were tested for pre-isotropic compatibility and optimization of the formulations by using DoE software. Dispersibility, self-emulsifying duration, mean globule size, and stability were determined by a heating-cooling cycle and phase separation. Methods: Self-nano emulsifying systems were created into free-flowing granules by adsorbing using the ratios of aerosil 200, sylysia 350, 550, and 730 as porous carriers and neusilin as an adsorbing agent. The FT-IR study assessed the drug's compatibility with various excipients and confirm no interaction. The produced granules were analyzed using differential scanning calorimetry, dissolution profile, and other flow property measures. The SEM examination revealed no evidence of drug precipitation on the carrier's surface. Self-nano emulsifying tablets were prepared through direct compression and changed by adding hydrophilic polymers like Avicel 112 and cross-povidone. Results: The tablets produced had a round form, a pleasing appearance, less friability, and a faster rate of disintegration. The X-RD was used to characterize the physical properties of the pure drug and S-SEDDS, which determined that both the pharmaceutical and formulations were amorphous. Comparative dissolving testing with capsules in SGF pH 1.2 and phosphate buffer pH 6.8 revealed a significant increase in drug dissolution over the pure drug. Conclusion: The study signifies the chosen drug using S-SEDDS improved its biopharmaceutical performance significantly, which may be relevant to other drugs with similar properties.

Recent Advancement in Self Emulsifing Drug Delivery System

“…The modification of PLGA NPs with lactoferrin or anti-transferrin receptor monoclonal antibody increased BBB crossing in vitro [45] [60] . Similarly, SLNs effectively crossed cerebral vascular endothelial cells and conjugation with apolipoprotein E or transferrin significantly increased cell uptake [13] [51] . In a multicellular BBB model consisting of primary rat brain endothelial cells, astrocytes, and pericytes, SLNs penetrated the barrier and targeting was increased over 3-fold by surface modification with apolipoprotein E [54] .…”

“…Remarkably, 20 mg/mL PLGA NPs was not toxic to 16HBE cells [50] . Similarly, the application of SLNs to human hCMEC/D3 cerebral vascular endothelial cells, SH-SY5Y cells, primary rodent astrocytes, and brain endothelial cells or mouse BV-2 microglia, brain endothelial cells, and embryonic fibroblasts did not affect cell viability [13][51][52][53][54] [55] .…”

“…Ethmoidal arteries, which originate in the ophthalmic and internal carotid arteries, provide an abundant blood supply to the nose [8]. Substances can enter the central nervous system via the perivascular areas surrounding these arteries [5,11].Studies comparing intranasal and arterial administration in animals have shown that substances administered in the former route enter the cerebral perivascular spaces within 20 minutes [16], are found in greater concentrations in the dura mater and circle of Willis [17], and are found in greater concentrations in the deep and superficial cervical nodes of rats [95], indicating that they may be transported via lymphatic drainage from the nasal passages and CSF. The maxillary, ophthalmic, and facial arteries, all of which are branches of the carotid artery, are the primary routes through which intranasal medicines reach the central nervous system.…”

“…To address these issues, new formulations have been created, with lipidic nanosystems receiving increasing attention in recent years. The primary objective of these systems is to maintain the solubility of lipophilic substances in aqueous environments, such as the GIT or nasal mucosa [11]. Lipophilic BCS class II and IV medicines can be easily included into selfemulsifying drug delivery systems (SEDDS) [12,13], a form of lipidic nanosystem.…”

“…The primary objective of these systems is to maintain the solubility of lipophilic substances in aqueous environments, such as the GIT or nasal mucosa [11]. Lipophilic BCS class II and IV medicines can be easily included into selfemulsifying drug delivery systems (SEDDS) [12,13], a form of lipidic nanosystem. More research into SEDDS technology [14] has been prompted by the commercialization of drugs like SandimmunNeoral®, (cyclosporin A) by Novartis Pharmaceuticals (USA), Norvir® by AbbVie Inc. (North Chicago, IL, USA), and Fortovase® by Roche (Basel, Switzerland).…”