Loading and Controlled Release of Poorly Water-Soluble Drug Telmisartan from Porous Silicon Microparticles

被引：1
作者：
Sharma, Chetan [1 ]
Maniya, Nalin H. [2 ]
Desai, Meghal A. [1 ]
Patel, Sanjaykumar R. [1 ]
机构：
[1] Sardar Vallabhbhai Natl Inst Technol, Chem Engn Dept, Surat, India
[2] Gujarat Biotechnol Res Ctr, Ghandhinagar 382011, Gujarat, India
来源：
SILICON | 2021年 / 13卷 / 02期
关键词：
Telmisartan; Electrochemical etching; Drug delivery; Drug loading; Release kinetics; GRAFTED MESOPOROUS SILICA; DELIVERY-SYSTEM; DISSOLUTION; BIOAVAILABILITY; NANOPARTICLES; ENHANCEMENT; ACYCLOVIR; CARRIERS; MICRO; SIZE;
D O I：
10.1007/s12633-020-00465-7
中图分类号：
O64 [物理化学（理论化学）、化学物理学];
学科分类号：
070304 ; 081704 ;
摘要：
Objective To prepare porous silicon microparticles by electrochemical etching process and study telmisartan loading and release kinetics to develop controlled drug delivery system. Method A 50 mA/cm(2) of current density was applied for 180 s in HF:ethanol (2:4) solution for the etching of silicon wafer. The silicon film was fractured by probe sonication at 20 kHz of frequency and 750 W powers for 120 s to make the micro-sized particles. Drug-loading was carried out by taking 1 M sodium hydroxides solution and in vitro release of telmisartan was investigated using various models, such as zero order, first order, Hixson Crowell, Korsmeyer-Peppas, and Higuchi diffusion model. Results A telmisartan loaded native porous silicon microparticles (TEL-PSi) allowed a very high drug loading up to 58.39 micrograms as compared to telmisartan loaded thermally oxidized porous silicon (TEL-TOPSi) (28.14 micrograms). TEL-TOPSi showed controlled release as compare to TEL-PSi. The release rate of TEL-TOPSi and TEL-PSi was 47% and 77% after 5 h respectively. The Korsmeyer-Peppas model was selected based on its excellent fitting to the release data among all models and indicates diffusion-based release. Conclusion Telmisartan loading and its release kinetics was studied successfully on porous silicon micro particles. TEL-TOPSi micro particles can be used for controlled drug delivery system for poorly water-soluble active pharmaceutical ingredients.
引用
收藏
页码：605 / 612
页数：8
相关论文
共 33 条
[1]   A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY [J].
AMIDON, GL ;
LENNERNAS, H ;
SHAH, VP ;
CRISON, JR .
PHARMACEUTICAL RESEARCH, 1995, 12 (03) :413-420
[2]   Porous silicon in drug delivery devices and materials [J].
Anglin, Emily J. ;
Cheng, Lingyun ;
Freeman, William R. ;
Sailor, Michael J. .
ADVANCED DRUG DELIVERY REVIEWS, 2008, 60 (11) :1266-1277
[3]   Nanocrystallization by Evaporative Antisolvent Technique for Solubility and Bioavailability Enhancement of Telmisartan [J].
Bajaj, Amrita ;
Rao, Monica R. P. ;
Pardeshi, Amol ;
Sali, Dhanesh .
AAPS PHARMSCITECH, 2012, 13 (04) :1331-1340
[4]   Nanostructure-coated diclofenac-loaded microparticles:: Preparation, morphological characterization, in vitro release and in vivo gastrointestinal tolerance [J].
Beck, RCR ;
Pohlmann, AR ;
Benvenutti, EV ;
Costa, TD ;
Guterres, SS .
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY, 2005, 16 (6A) :1233-1240
[5]   Functional hydrophobin-coating of thermally hydrocarbonized porous silicon microparticles [J].
Bimbo, Luis M. ;
Makila, Ermei ;
Raula, Janne ;
Laaksonen, Timo ;
Laaksonen, Paivi ;
Strommer, Katharina ;
Kauppinen, Esko I. ;
Salonen, Jarno ;
Linder, Markus B. ;
Hirvonen, Jouni ;
Santos, Helder A. .
BIOMATERIALS, 2011, 32 (34) :9089-9099
[6]   Nanonization strategies for poorly water-soluble drugs [J].
Chen, Huabing ;
Khemtong, Chalermchai ;
Yang, Xiangliang ;
Chang, Xueling ;
Gao, Jinming .
DRUG DISCOVERY TODAY, 2011, 16 (7-8) :354-360
[7]   Design, characterization and in vivo evaluation of nanostructured lipid carriers (NLC) as a new drug delivery system for hydrochlorothiazide oral administration in pediatric therapy [J].
Cirri, Marzia ;
Maestrini, Lavinia ;
Maestrelli, Francesca ;
Mennini, Natascia ;
Mura, Paola ;
Ghelardini, Carla ;
Mannelli, Lorenzo Di Cesare .
DRUG DELIVERY, 2018, 25 (01) :1910-1921
[8]   Modeling and comparison of dissolution profiles [J].
Costa, P ;
Manuel, J ;
Lobo, S .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2001, 13 (02) :123-133
[9]  
Halimaoui A., 1995, POROUS SILICON SCI T, P33, DOI [10.1007/978-3-662-03120-93, DOI 10.1007/978-3-662-03120-93]
[10]   Influence of pore size of MCM-41 matrices on drug delivery rate [J].
Horcajada, P ;
Rámila, A ;
Pérez-Pariente, J ;
Vallet-Regí, M .
MICROPOROUS AND MESOPOROUS MATERIALS, 2004, 68 (1-3) :105-109
1234