Effect of organogel components on in vitro nasal delivery of propranolol hydrochloride

Abstract

The purpose of this research was to evaluate in vitro transnasal sustained-release ability of sorbitan monostearate (SMS) organogels in isopropyl myristate (IM). Organogels were prepared containing SMS (2.5%-20%) and water (5%-25%) in IM and analyzed microscopically for phase behavior. The effect of Tween surfactants on gel strength and in vitro nasal diffusion of propranolol is reported. The in vitro nasal release retardant effect of SMS and Tween 20 was investigated using factorial design. The microscopic changes in structure of organogel during in vitro nasal diffusion were studied. The water-holding capacity of SMS organogels in IM increased with SMS concentration. The release retardant effect with incorporation of cosurfactant was of the order of Tween 80 > Tween 60 > Tween 20. Gel strengthening and increased viscosity were evident with increased concentration of SMS and Tween 20. The 3-dimensional network of SMS molecules controls the diffusional drug release. The organogel system on nasal mucosa during diffusion is dynamic in nature and changes continuously with the time of diffusion. The water penetration in the organogel network results in percolation and emulsification of organogel, thus affecting the release. Organogels provided an effective barrier for diffusion of propranolol. The surface epithelium lining and the granular cellular structure of treated nasal mucosa were intact.

Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

“…Organogels have been investigated in fields as diverse as molecular photonics [1], art conservation [2] and food industry [3]. In the area of pharmaceutical sciences, organogels have only received a marked interest in recent years [4][5][6]. They have been tested with more or less success for the administration of inflammatory/analgesic drugs [7][8][9], cardiovascular drugs [4], antipsychotics [10] as well as nucleic acids [11] and peptides [12] by the transdermal, rectal, oral and buccal routes.…”

“…They have been tested with more or less success for the administration of inflammatory/analgesic drugs [7][8][9], cardiovascular drugs [4], antipsychotics [10] as well as nucleic acids [11] and peptides [12] by the transdermal, rectal, oral and buccal routes. In drug delivery, organogels are generally prepared using biocompatible and safe gelating molecules such as lecithin [8,[13][14][15], sorbitan monostearate (SMS) [4,12,16] and amino acid derivatives [17]. A promising avenue for organogels lies in their use as depot formulations following parenteral extravascular injection.…”

Nasal-nanotechnology: revolution for efficient therapeutics delivery

“…These systems are not of much interest until the recent advancement in precise dosing devices. The advantages of NGs take account of reduced mucociliary clearance due to elevated viscosity, reduction in taste impact due to reduced post-nasal drip towards nasopharynx, reduced irritation due to soothing/emollient excipients and target delivery to mucosa for better absorption (Pisal et al, 2004a;Alsarra et al, 2009;Al-Ghananeem et al, 2011). Deposition of NGs in the nasal cavity is influenced by the mode of administration, because elevated viscosities of these systems responds in terms of deprived spreading abilities.…”

Thermoreversible Nasal In situ Gel of Venlafaxine Hydrochloride: Formulation, Characterization, and Pharmacodynamic Evaluation

“…The mucosa was stored in normal saline solution. After the removal of blood and bony cartilage from the mucosal membrane, it was ready for use (16). Franz diffusion cells were placed on six station magnetic stirring unit.…”