Utilization of propranolol hydrochloride mucoadhesive invasomes as a locally acting contraceptive: in-vitro, ex-vivo, and in-vivo evaluation

Abstract

It was found that propranolol hydrochloride (PNL), which is a beta-blocker used for hypertension treatment, has a potent spermicidal activity through local anesthetic activity or beta-blocking effect on sperm cells subsequently it could be used as a contraceptive remedy. This study aimed to entrap PNL into invasomes (INVs) and then formulate it as a locally acting contraceptive gel. PNL-loaded mucoadhesive INVs were prepared via the thin-film hydration technique. The D-optimal design was utilized to fabricate INVs employing lipid concentration (X 1 ), terpenes concentration (X 2 ), terpenes type (X 3 ), and chitosan concentration (X 4 ) as independent variables, while their impact was observed for entrapment efficiency percent (Y 1 ; EE%), particle size (Y 2 ; PS), zeta potential (Y 3 ; ZP), and amount of drug released after 6 h (Y 4 ; Q6h). Design Expert® was bestowed to nominate the desired formula. The selected INV was subjected to further studies and formulated into a mucoadhesive gel for ex-vivo and in-vivo investigations. The optimum INV showed a spherical shape with EE% of 65.01 ± 1.24%, PS of 243.75 ± 8.13 nm, PDI of 0.203 ± 0.01, ZP of 49.80 ± 0.42 mV, and Q6h of 53.16 ± 0.73%. Differential scanning calorimetry study asserted the capability of INVs to entrap PNL. Permeation studies confirmed the desired sustained effect of PNL-loaded INVs-gel compared to PNL-gel, INVs, and PNL solution. Sperm motility assay proved the potency of INVs-gel to inhibit sperm motility. Besides, the histopathological investigation verified the tolerability of the prepared INVs-gel. Taken together, the gained data justified the efficacy of PNL-loaded INVs-gel as a potential locally acting contraceptive.

Exploring the Synergistic Effect of Bergamot Essential Oil with Spironolactone Loaded Nano-Phytosomes for Treatment of Acne Vulgaris: In Vitro Optimization, In Silico Studies, and Clinical Evaluation

“…The optimum formula stability was examined to investigate the degree of drug leakage, vesicles’ growth, sedimentation, or any other physical variation. The optimized formula was left in the refrigerator for three months and then evaluated by comparing the responses of the stored formula, including EE%, PS, PDI, and ZP, with the fresh formula [ 39 ].…”

Lyophilized Nasal Inserts of Atomoxetine HCl Solid Lipid Nanoparticles for Brain Targeting as a Treatment of Attention-Deficit/Hyperactivity Disorder (ADHD): A Pharmacokinetics Study on Rats

“…The ZP was carried out in deionized water by detecting the electrophoretic mobility of the charged solid lipid nanoparticles in an electrical field, and that indicated their permeation behavior by studying their colloidal property and stability. PDI values less than 0.5 are more common to monodisperse samples, while values larger than 0.7 are common to a broad size (e.g., polydisperse) distribution of particles [ 57 , 58 ]. The results are the mean values of three runs ± SD.…”

“…Finally, the stained samples were visualized using transmission electron microscopy. (JEM 1230, Jeol, Tokyo, Japan) [ 58 ].…”

Sertaconazole-Nitrate-Loaded Leciplex for Treating Keratomycosis: Optimization Using D-Optimal Design and In Vitro, Ex Vivo, and In Vivo Studies

“…The optimized formula was kept at 4 °C temperature for 3 months and then examined by comparing the PS, PDI, and ZP of the stored formula with the fresh formula. Additionally, the system was visually observed for sedimentation [ 24 ].…”