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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제51권 제3호
- 발행연도
- 2021.1
- 수록면
- 297 - 310 (14page)
이용수
초록· 키워드
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Purpose Aprepitant (APRT), a selective neurokinin 1 antagonist, is clinically used in the prevention of acute and delayed chemotherapy-induced nausea and vomiting. The low solubility of APRT, which limits its oral bioavailability, is overcome by nanonization. This study aimed to design and evaluate novel in vitro and in vivo chitosan (CS)?polyethylene glycol (PEG)-coated cyclodextrin (CD) nanoparticles and nanocapsules to enhance the solubility and oral bioavailability of APRT. Methods A novel amphiphilic CD derivative with alkyl chains of 9 carbons (ACD-C9) was synthesized to form nanoparticles and nanocapsules by using nanoprecipitation. The nanocarriers were coated with the CS?PEG conjugate to increase their biological interaction with cell membranes via the positive charge and penetration-enhancer properties of CS. The nanosystems were evaluated for particle size, surface charge, drug loading, imaging, release, cell culture, and oral bioavailability in an animal model. Results The CS?PEG-coated nanosystems had particle size of 400?550 nm, a narrow polydispersity index, positive zeta potential, and favorable drug loading (55 and 93% for nanoparticles and nanocapsules, respectively). Sustained release was observed within 24 h. Blank nanoparticles and nanocapsules were non-cytotoxic against the L929 cell line. The intestinal permeability of the nanocarriers was 2?threefold (2-3 fold) higher than that of the drug solution, and the nanocapsules afforded the highest APRT permeability through Caco-2 cells. Oral bioavailability studies in rats revealed comparable degree of drug absorption between nanocapsules and commercial APRT products. Conclusion Oral ACD-C9 nanocapsules have the potential for the treatment of chemotherapy-induced nausea and vomiting.
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참고문헌 (58)
참고문헌 신청
Adel N / 2017 / Overview of chemotherapy-induced nausea and vomiting and evidence-based therapies / Am J Manage Care 23:S259~S265
Aktas Y / 2005 / Preparation and in vitro evaluation of chitosan nanoparticles containing a caspase inhibitor / Int J Pharm 298:378~383
Aktas Y / 2015 / Amphiphilic cyclodextrins as enabling excipients for drug delivery and for decades of scientific collaboration: tribute to a distinguished scientist, French representative and friend—a historical perspective / J Drug Deliv Sci Technol 30:261~265
Attari Z / 2015 / Formulation and characterisation of nanosuspensions of BCS class II and IV drugs by combinative method / J Exp Nanosci 11:276~288
Bilensoy E / 2009 / Recent advances and future directions in amphiphilic cyclodextrin nanoparticles / Expert Opin Drug Deliv 6:1161~1173
Aktas Y / 2005 / Preparation and in vitro evaluation of chitosan nanoparticles containing a caspase inhibitor / Int J Pharm 298:378~383
Aktas Y / 2015 / Amphiphilic cyclodextrins as enabling excipients for drug delivery and for decades of scientific collaboration: tribute to a distinguished scientist, French representative and friend—a historical perspective / J Drug Deliv Sci Technol 30:261~265
Attari Z / 2015 / Formulation and characterisation of nanosuspensions of BCS class II and IV drugs by combinative method / J Exp Nanosci 11:276~288
Bilensoy E / 2009 / Recent advances and future directions in amphiphilic cyclodextrin nanoparticles / Expert Opin Drug Deliv 6:1161~1173
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