Preparation of melatonin novel-mucoadhesive nanoemulsion used in the treatment of depression

被引：12

作者：

Ahmad, Niyaz ^{[1
]}

Khalid, Mohammed Saifuddin ^{[2
]}

Al Ramadhan, Ayman Makki ^{[1
]}

Alaradi, Mohammed Zaki ^{[1
]}

Al Hammad, Mohammed Riyad ^{[1
]}

Ansari, Khalid ^{[3
]}

Alqurashi, Yousef D. ^{[3
]}

Khan, Mohd Faiyaz ^{[4
]}

Albassam, Ahmed A. ^{[4
]}

Ansari, Mohammad Javed ^{[5
]}

Akhtar, Sultan ^{[6
]}

Dilshad, Mubah ^{[7
]}

机构：

[1] Imam Abdulrahman Bin Faisal Univ, Coll Clin Pharm, Dept Pharmaceut, POB 1982, Dammam 31441, Saudi Arabia

[2] Imam Abdulrahman Bin Faisal Univ, Coll Clin Pharm, Dept Pharmacol, Dammam, Saudi Arabia

[3] Imam Abdulrahman Bin Faisal Univ, Coll Appl Med Sci, Dept Resp Care, Dammam, Saudi Arabia

[4] Prince Sattam Bin Abdulaziz Univ, Coll Pharm, Dept Clin Pharm, Alkharj, Saudi Arabia

[5] Prince Sattam Bin Abdulaziz Univ, Coll Pharm, Dept Pharmaceut, Alkharj, Saudi Arabia

[6] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Phys, POB 1982, Dammam 31441, Saudi Arabia

[7] Era Med Univ, Coll Med, Lucknow 226003, Uttar Pradesh, India

来源：

POLYMER BULLETIN | 2023年 / 80卷 / 07期

关键词：

Melatonin; Ultrasonication technique; Mucoadhesive nanoemulsion; Three-factor four-level central-composite design (CCD); UHPLC-MS/MS-based bioanalytical method; Brain bioavailability; Depression study; COATED PLGA NANOPARTICLES; FORCED SWIMMING TEST; CYTOTOXICITY; BRAIN; MICE; BIOAVAILABILITY; QUANTIFICATION; AGOMELATINE; GENERATION; SECRETION;

D O I：

10.1007/s00289-022-04436-3

中图分类号：

O63 [高分子化学（高聚物）];

学科分类号：

070305 ; 080501 ; 081704 ;

摘要：

In this current research work has a main aim to develop a novel Melatonin (MLT: BCS class II drug)-loaded nanoemulsion for the improvement in solubility. A developed novel-NE was to evaluate and compare the efficacy of Melatonin-loaded mucoadhesive nanoemulsion (CS-MLT-NE) with Melatonin-loaded nanoemulsion (MLT-NE) and MLT-solution (MLT-S) pharmacodynamically and also determine the quantity of MLT in the brain after the nasal administration. MLT-NE was prepared with the help of an advanced ultrasonication method after the screening of excipients and the development of pseudoternary phase diagram study. We got the optimized nanoformulation via three-factor four-level central-composite design (CCD). We optimized %oil, %S-mix, and sonication time (second) based on selected independent variables. Independent and dependent variables were selected and optimized on the basis constraints oil (2.0%), 10%S-mix, and 120 s sonication time. The dependent variables found the experimental their values 49.37 +/- 4.09 nm (Y-1: Globule size), 0.257 +/- 0.0004 (Y-2: PDI), - 16.20 +/- 1.10 mV (Y-3: Zeta Potential), and 98.03 +/- 0.59% (Y-4: %Transmittance), respectively. The shape of optimized-MLT-NE was found spherical with the pH, viscosity, and drug content (7.40 +/- 0.08, 37.86 +/- 7.01 cp, and 98.27 +/- 0.17%), respectively. Zeta-Potential of CS-MLT-NE was altered from -ve to +ve after the addition of CS followed small increment of globule-size. CS-MLT-NE showed the great mucoadhesive nature as compared to MLT-NE, and MLT-S with a retention time of 0.641 min and m/z of 233.20/174.20 for MLT. A linear range was established from 0.50 to 1500.0 ng mL(-1) with %accuracy (92.41-98.61%) and inter- and intraday %precision (2.49-4.93%). C-max was enhanced (AUC)(0-24) which was greatly significant (p < 0.001) in the rat's brain when it compared with i.n. and intravenous-treated group. Moreover, FST (forced swimming, climbing, and immobility) and locomotor activity test of CS-MLT-NE (i.n.) showed highly improved behavioral analysis as compared to the MLT-NE and MLT-S after 24.0 h of study. CS-MLT-NE showed highly significant role (p < 0.001) for the improvement in brain bioavailability and treatment of depression. [GRAPHICS] .

引用

页码：8093 / 8132

页数：40

共 64 条

[1] Quantification and Evaluations of Catechin Hydrate Polymeric Nanoparticles Used in Brain Targeting for the Treatment of Epilepsy [J].