Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation

被引:10
|
作者
Begum, M. Yasmin [1 ]
M. Osmani, Riyaz Ali [2 ]
Alqahtani, Ali [3 ]
Ghazwani, Mohammed [4 ]
Hani, Umme [1 ]
Ather, Hissana [4 ]
Atiya, Akhtar [5 ]
Rahamathulla, Mohamed [1 ]
Siddiqua, Ayesha [6 ]
机构
[1] King Khalid Univ, Coll Pharm, Dept Pharmaceut, Abha, Saudi Arabia
[2] JSS Acad Higher Educ & Res, JSS Coll Pharm, Dept Pharmaceut, Mysuru, Karnataka, India
[3] King Khalid Univ, Coll Pharm, Dept Pharmacol, Abha, Saudi Arabia
[4] King Khalid Univ, Coll Pharm, Dept Pharmaceut Chem, Abha, Saudi Arabia
[5] King Khalid Univ, Coll Pharm, Dept Pharmacognosy, Abha, Saudi Arabia
[6] King Khalid Univ, Coll Pharm, Dept Clin Pharm, Abha, Saudi Arabia
来源
PLOS ONE | 2022年 / 17卷 / 04期
关键词
RHEUMATOID-ARTHRITIS; SKIN PERMEATION; PLASMA; PHARMACOKINETICS; OSTEOARTHRITIS; MICROEMULSION; STABILITY; COMPLEX;
D O I
10.1371/journal.pone.0264518
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Celecoxib (CLB) is a highly hydrophobic selective cyclo-oxygenase inhibitor with high plasma protein binding and undergoes extensive hepatic metabolism. CLB is highly effective in the treatment of osteo and rheumatoid arthritis as first line therapy but produces severe gastro-intestinal toxicities and cardiovascular side effects. In this research, stealth liposomes of CLB were developed with the intention to reduce the side effects and increase the accumulation of drug in the sites of inflammation. Stealth liposomes were prepared by thin film hydration technique using distearoylphosphatidylcholine and PE-PEG 2000 with variable amounts of cholesterol and characterized. The effects of various lipids such as hydrogenated soy phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoylphosphatidylcholine and cholesterol content on % drug encapsulation was investigated. The optimized stealth liposomes were characterized by FT-IR and DSC for possible drug excipients interaction. Pharmacokinetics, pharmacodynamics and biodistribution studies were carried out for the stealth liposomes. The results revealed that the stealth liposomes reduced the inflammation to the larger magnitude and have also sustained the magnitude when compared to free drug along with maximum analgesic response. Higher elimination half-life, AUC, MRT and lowered clearance rate denotes the extended bioavailability of the drug in blood. Biodistribution studies revealed that stealth liposomes extend the circulation time of liposomes in blood by decreasing opsonisation and be less concentrated in kidney, thereby reducing the toxicities to RES and renal organs and facilitate the drug accumulation in the area of inflammation. Our results indicated that CLB, without the requirement of modifications to enhance solubilisation, can be encapsulated and released from liposomal formulations. This new-fangled drug delivery approach may be used to circumvent the low bioavailability and toxic side effects of oral CLB formulations.
引用
收藏
页数:22
相关论文
共 50 条
  • [1] Formulation and development of floating capsules of celecoxib: In vitro and in vivo evaluation
    Ali J.
    Arora S.
    Ahuja A.
    Babbar A.K.
    Sharma R.K.
    Khar R.K.
    [J]. AAPS PharmSciTech, 8 (4) : E1 - E8
  • [2] Formulation and Development of Floating Capsules of Celecoxib: In Vitro and In Vivo Evaluation
    Ali, Javed
    Arora, Shweta
    Ahuja, Alka
    Babbar, Anil K.
    Sharma, Rakesh K.
    Khar, Roop K.
    [J]. AAPS PHARMSCITECH, 2007, 8 (04):
  • [3] Formulation development and in vivo evaluation of liposomal paclitaxel
    Kan, P
    Tsao, CW
    Chen, WK
    Wang, AJ
    [J]. JOURNAL OF LIPOSOME RESEARCH, 2003, 13 (01) : 69 - 69
  • [4] Development of a stealth liposomal formulation of d-Ino as 5-FU modulator: in vitro and in vivo study
    Fanciullino, Raphaelle
    Giacometti, Sarah
    Fina, Frederic
    Aubert, Claude
    Piccerelle, Philippe
    Ciccolini, Joseph
    [J]. CANCER RESEARCH, 2006, 66 (08)
  • [5] In Vitro and In Vivo Evaluation of Lipofufol, a New Triple Stealth Liposomal Formulation of Modulated 5-Fu: Impact on Efficacy and Toxicity
    Fanciullino, Raphaelle
    Mollard, Severine
    Giacometti, Sarah
    Berda-Haddad, Yael
    Chefrour, Mohamed
    Aubert, Claude
    Iliadis, Athanassios
    Ciccolini, Joseph
    [J]. PHARMACEUTICAL RESEARCH, 2013, 30 (05) : 1281 - 1290
  • [6] In Vitro and In Vivo Evaluation of Lipofufol, a New Triple Stealth Liposomal Formulation of Modulated 5-Fu: Impact on Efficacy and Toxicity
    Raphaelle Fanciullino
    Séverine Mollard
    Sarah Giacometti
    Yael Berda-Haddad
    Mohamed Chefrour
    Claude Aubert
    Athanassios Iliadis
    Joseph Ciccolini
    [J]. Pharmaceutical Research, 2013, 30 : 1281 - 1290
  • [7] Formulation, in vitro and in vivo evaluation of celecoxib nanosponge hydrogels for topical application
    Gangadharappa, H. V.
    Prasad, Sarat M. Chandra
    Singh, Rudra Pratap
    [J]. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2017, 41 : 488 - 501
  • [8] Liposomal Gels for Site-Specific, Sustained Delivery of Celecoxib: In Vitro and In Vivo Evaluation
    Fetih, Gihan
    Fathalla, Dina
    El-Badry, Mahmoud
    [J]. DRUG DEVELOPMENT RESEARCH, 2014, 75 (04) : 257 - 266
  • [9] Quality by Design-Steered Development of Stealth Liposomal Formulation of Everolimus: A Systematic Optimization and Evaluation
    Kaur, Simranjeet
    Sidhu, Rajveer
    Singh, Dilpreet
    [J]. CURRENT DRUG METABOLISM, 2024,
  • [10] Stable and sustained release liposomal formulations of celecoxib: In vitro and in vivo anti-tumor evaluation
    Riahi, M. Matbou
    Sahebkar, A.
    Sadri, K.
    Nikoofal-Sahlabadi, S.
    Jaafari, M. R.
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2018, 540 (1-2) : 89 - 97