Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier

Abstract

One drawback of traditional forms of medical ocular dosage is drug dilution by tear; moreover, drugs are rapidly drained away from pre-corneal cavity by tear flow and lacrimo-nasal drainage. Prolonging contact time with different strategies and mucoadhesive vehicles will help to continuously deliver drugs to the eyes. For this study, we prepared and evaluated the effects of a nanostructure lipid carrier (NLC) on propranolol hydrochloride as a hydrophilic drug model for rabbit corneal permeation. Propranolol hydrochloride NLC was prepared using cold homogenization. The lipid was melted, then the drug and surfactant were dispersed and stirred into the melted lipid. This fused lipid phase was scattered in aqueous solution containing the cosurfactant at 4 °C and then homogenized. We evaluated particle size, drug loading, drug release, and NLC permeability through rabbit cornea as well as the formula’s effect on the cornea. Our results show that drug loading efficiency depended on the surfactant/lipid ratio (S/L) and the percentages of liquid lipid and Transcutol (Gattefosse, Saint-Priest, France) (as solubilizer). Drug release data were evaluated with the Higuchi model and a significant correlation was shown between the S/L ratio and the amount of drug released after 4 and 48 h. NLC formulations improved propranolol hydrochloride permeation. We conclude that the effect of the NLC formulations was due to mucoadhesive and film forming properties.

In‐vitro and in‐vivo evaluation of chitosan‐based thermosensitive gel containing lorazepam NLCs for the treatment of status epilepticus

“…However, while increasing the oil content had no significant effect on EE, a more homogeneous entrapment of LZM throughout the systems could result in the decline of RE [29]. Similar results were obtained by Sharif Makhmal Zadeh et al [43], who proved that increasing the oil content resulted in the decrease of the drug release rate. Conversely, the increment of the surfactant concentration (though not significant) in the formulation led to the increase of RE, possibly due to the increased drug solubility in the water phase [44].…”

Nanocarriers for ocular drug delivery: current status and translational opportunity

“…21,[45][46][47][48][49][50][51][52][53][54][55][56][57][58][59] Some examples of recent ndings with the above-mentioned nanocarriers for the treatment of ophthalmic diseases are compiled in Table 3. [60][61][62][63][64][65][66][67][68][69][70][71][72][73][74][75][76][77][78][79]…”

Sunitinib-Loaded MPEG-PCL Micelles for the Treatment of Age-Related Macular Degeneration

“…The in vitro drug release included a comparison of the pure SM drug solution and the SM-MPEG-PCL formulation by the use of a dialysis bag (MWCO 14,000 Da) [30]. In preparation for the loading of both the sunitinib solution and the SM-MPEG-PCL formulation, the release medium was prepared by the addition of PBS with a pH adjusted to 7.4 [31], along with a Tween 80 solution (0.1% v/v). The release medium was further optimized under magnetic stirring at 100 rpm with a constant temperature of 37 • C. Out of the 5 mL of the release medium, approximately 200 µL of each formulation were taken and subsequently replaced with 200 µL of the release medium at time intervals of 0.25, 0.5, 1, 2, 3, 4, 5, and 6 h for the initial day and every 24 h for the next seven days.…”

“…In a 96-well plate, cells were seeded at a density of 5000 cells per well supplemented with a medium consisting of 200 µL of DMEM F12 and a 10% FBS solution. Cells were then allowed to grow in a 5% atmosphere, 37 • C, CO 2 incubator for 24 h to ensure the proper attachment of the cells to the bottom of the well plates [31]. Following initial incubation, cells were then treated with dilutions of 0.001, 0.01, 0.1, 1, 10, and 20 µM of the drug solution, as well as the SM-MPEG-PCL formulation in quadruplicate.…”