Loratadine oral bioavailability enhancement via solid dispersion loaded oro-dispersible films: Formulation, characterization and pharmacokinetics

doi:10.1016/j.colsurfb.2023.113526

	Loratadine oral bioavailability enhancement via solid dispersion loaded oro-dispersible films: Formulation, characterization and pharmacokinetics
	Islam, Nayyer 7,8; Khan, Naveed Ullah 8; Razzaq, Anam 6; Menaa, Farid 4,5; Khan, Zaheer Ullah 3; Hussain, Abid 9; Rehman, Saif Ur 9; Iqbal, Haroon 2; Ni, Jiang 1
刊名	COLLOIDS AND SURFACES B-BIOINTERFACES
	2023-10-01
卷号	230
关键词	Loratadine Solid dispersion Oro-dispersible film Bioavailability Urticaria
ISSN号	0927-7765
DOI	10.1016/j.colsurfb.2023.113526
通讯作者	Iqbal, Haroon(harooniqbal415@hotmail.com) ; Ni, Jiang(nj1876348@suda.edu.cn)
英文摘要	Loratadine (LRD) belongs to second-generation tricyclic H1 antihistamine class, known for its non-sedating properties in allergic reactions. H1 antihistamines avoid and block the responses to allergens or histamine in nose and conjunctivae, thereby abolishing itching, congestion and sneezing. LRD is a Biopharmaceutical Class System (BCS) class II drug with dissolution or solubility limited absorption which limited the oral bioavailability and therapeutic efficacy of LRD. To improve the oral bioavailability of LRD for allergic disease (urticaria) treatment, LRD solid dispersions (LRD-SDs) were integrating into oro-dispersible films (ODFs). LRD-SDs were prepared through hot-melt extrusion method (HME) using d-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS-1000), and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SP). Subsequently, LRD-SDs were incorporated in ODFs by solvent casting method. The physicochemical and mechanical properties of LRD solid dispersions-loaded oro-dispersible films (LRD-SDs-ODFs), were evaluated. The in-vitro dissolution, ex-vivo permeation, oral bioavailability, and pharmacodynamics studies were conducted to evaluate LRD-SDs-ODFs efficiency. LRD-SDs-ODFs showed superior solubility and in-vitro dissolution results compared to that of pure LRD (p < 0.05). The solubility of the LRD-SD coded as LTS-4 was 190 times higher than the pure drug in aqueous media. The average hydrodynamic particle size (PS), polydispersity index (PDI), and zeta potential (ZP) of SD particles were 76 +/- 2.1 nm, 0.20 +/- 0.08 and - 19.16 +/- 1.4 mV, respectively. Moreover, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results confirmed the amorphousness of LRD in LRD-SDs-ODFs. The permeability flux of LRD was 44.6 +/- 3.1 mu g/cm(2)/h from DPF-5 formulation. Likewise, in vivo oral bioavailability of DPF-5 in Sprague-Dawley rats was significantly increased (p < 0.05) compared to free LRD. Further, wheal area was reduced 20 % higher than LRD in 8 h (p < 0.05). Overall, LRD-SDs-ODFs considerably enhanced LRD solubility, dissolution rate, bioavailability, and antihistaminic efficacy. Our findings show that SDs-ODFs is an effective carrier system for delivering poorly soluble LRD.
资助项目	Wuxi municipal health commission youth research project[Q202230]
WOS关键词	IN-VIVO ; MICELLES ; EFFICACY ; DELIVERY ; VITRO ; TPGS
WOS研究方向	Biophysics ; Chemistry ; Materials Science
语种	英语
出版者	ELSEVIER
WOS记录号	WOS:001082184300001
资助机构	Wuxi municipal health commission youth research project
内容类型	期刊论文
源URL	[http://ir.hfcas.ac.cn:8080/handle/334002/133384]
专题	中国科学院合肥物质科学研究院
通讯作者	Iqbal, Haroon; Ni, Jiang
作者单位	1.Jiangnan Univ, Dept Pharm, Affiliated Hosp, Wuxi 214000, Peoples R China 2.Chinese Acad Sci, Univ Chinese Acad Sci, Canc Hosp, Zhejiang Canc Hosp,Inst Basic Med & Canc IBMC, Hangzhou 310022, Zhejiang, Peoples R China 3.COMSATS Univ, Dept Pharm, Abbottabad Campus, Lahore, Pakistan 4.Calif Innovat Corp, Dept Nanomed, San Diego, CA 92037 USA 5.Calif Innovat Corp, Dept Oncol, San Diego, CA 92037 USA 6.Soochow Univ, Coll Pharmaceut Sci, Suzhou 215123, Peoples R China 7.Govt Coll Univ Faisalabad, Fac Pharm, Faisalabad, Pakistan 8.Univ Chenab, Gujrat, Pakistan 9.Univ Poonch, Fac Med & Hlth Sci, Dept Pharm, Rawalakot 12351, Pakistan
推荐引用方式 GB/T 7714	Islam, Nayyer,Khan, Naveed Ullah,Razzaq, Anam,et al. Loratadine oral bioavailability enhancement via solid dispersion loaded oro-dispersible films: Formulation, characterization and pharmacokinetics[J]. COLLOIDS AND SURFACES B-BIOINTERFACES,2023,230.
APA	Islam, Nayyer.,Khan, Naveed Ullah.,Razzaq, Anam.,Menaa, Farid.,Khan, Zaheer Ullah.,...&Ni, Jiang.(2023).Loratadine oral bioavailability enhancement via solid dispersion loaded oro-dispersible films: Formulation, characterization and pharmacokinetics.COLLOIDS AND SURFACES B-BIOINTERFACES,230.
MLA	Islam, Nayyer,et al."Loratadine oral bioavailability enhancement via solid dispersion loaded oro-dispersible films: Formulation, characterization and pharmacokinetics".COLLOIDS AND SURFACES B-BIOINTERFACES 230(2023).