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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2016  >  34(2): 148-152

WANG Xiang, ZHANG Liangyu, DING Baoyue, CHEN Yang. Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 148-152. doi: 10.3969/j.issn.1006-0111.2016.02.013
Citation: WANG Xiang, ZHANG Liangyu, DING Baoyue, CHEN Yang. Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 148-152. doi: 10.3969/j.issn.1006-0111.2016.02.013
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Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study

doi: 10.3969/j.issn.1006-0111.2016.02.013
  • 1.

    No.98 Hospital of PLA, Huzhou 313000, China

  • 2.

    School of Medicine, Jiaxing College, Jiaxing 310014, China

  • Received Date: 2015-03-09
  • Rev Recd Date: 2016-01-12
  • Objective To prepare a novel drug delivery system camptothecin loaded nanogel(CPT-PPO gel), and investigate its contents, physical and chemical properties and in vitro transdermal permeability. Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems(CPT-PLGA-PAMAM, CPT-PP), in which the Poly lactic-co-glycolic acid(PLGA) was used to load camptothecin as the nucleus and the polyamidoamine(PAMAM) G3.0 was wrapped in the surface of PLGA as the shell. Then the oleic acid(OA) was connected to CPT-PP to obtain the surface modified drug delivery system(CPT-PLGA-PAMAM OA, CPT-PPO). HPLC was used to determine the content of camptothecin in nanoparticles, transmission electron microscopy was applied to identify the nanoparticles morphology, and laser analyzer was used to determine the particle size. The hydroxypropyl methylcellulose(HPMC) was added as the base for the preparation of the nanogel(CPT-PPO gel) at last. The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃, the average particle size was(246.7±5.4) nm and the encapsulation efficiency was up to(78.7±6.9)%. Comparing to the normal gel,(CPT gel), the cumulative penetration amount and the retention amount in the skin of the nanogels(CPT-PPO gel,CPT-PP gel) were significant higher(P<0.01), the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel(P<0.05). Conclusion After modified by OA, CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.
  • [1] Barry BW. Novel mechanisms and devices to enable successful transdermal drug delivery[J]. Eur J Pharm Sci, 2001, 14(2):101-114.
    [2] Prow TW, Grice JE, Lin LL, et al. Nanoparticles and microparticles for skin drug delivery[J]. Adv Drug Deliv Rev, 2011, 63(6):470-491.
    [3] Gupta M, Vyas SP. Development, characterization and in vivo assessment of effective lipidic nanoparticles for dermal delivery of fluconazole against cutaneous candidiasis[J]. Chem Phys Lipids, 2012, 165(4):454-461.
    [4] Bachhav YG, Mondon K, Kalia YN, et al. Novel micelle formulations to increase cutaneous bioavailability of azole antifungals[J]. J Control Release, 2011, 153(2):126-132.
    [5] Vijayan V, Reddy KR, Sakthivel S, et al. Optimization and charaterization of repaglinide biodegradable polymeric nanoparticle loaded transdermal patchs:in vitro and in vivo studies[J]. Colloids Surf B Biointerfaces, 2013, 1(111):150-155.
    [6] Agrawal U, Mehra NK, Gupta U et al. Hyperbranched dendritic nano-carriers for topical delivery of dithranol[J]. J Drug Target,2013, 21(5):497-506.
    [7] Chen Y, Wang M, Fang L. Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems[J]. Drug Deliv, 2013, 20(5):199-209.
    [8] Rancan F, Papakostas D, Hadam S, et al. Investigation of polylactic acid(PLA) nanoparticles as drug delivery systems for local dermatotherapy[J]. Pharm Res, 2009, 26(8):2027-2036.
    [9] Shah PP, Desai PR, Channer D, et al. Enhanced skin permeation using polyarginine modified nanostructured lipid carriers[J]. J Controlled Release, 2012, 161(3):735-745.
    [10] Shah PP, Desai PR, Patel AR, et al. Skin permeating nanogel for the cutaneous co-delivery of two anti-inflammatory drugs[J]. Biomaterials, 2012, 33(5):1607-1617.
    [11] Yang Y, Sunoqrot S, Stowell C, et al. Effect of size, surface charges, and hydrophobicity of poly(amidoamine) dendrimers on their skin penetration[J]. Biomacromolecules,2012, 13(7):2154-2162.
    [12] O'Leary J, Muggia FM. Camptothecins:a review of their development and schedules of administration[J]. Eur J Cancer, 1998,34(10):1500-1508.
    [13] Min KH, Park K, Kim YS, et al. Hydrophobically modified glycol chitosan nanoparticles-encapsulated camptothecin enhance the drug stability and tumor targeting in cancer therapy[J]. J Control Release,2008, 127(3):208-218.
    [14] Andrew J. Jennifer K. Carmen J, et al. Convection-enhanced delivery of camptothecin-loaded polymer nanoparticles for treatment of intracranial tumors[J]. Drug Deliv Transl Res,2011,1(1):34-42.
    [15] Castillo PM, de la Mata M, Casula MF, et al. PEGylated versus non-PEGylated magnetic nanoparticles as camptothecin delivery system[J]. Beilstein J Nanotechnol, 2014, 5:1312-1319.
    [16] Zhang L, Hu Y, Jiang X, et al. Camptothecin derivative-loaded poly(caprolactone-co-lactide)-b-PEG-b-poly(caprolactone-co-lactide) nanoparticles and their biodistribution in mice[J]. J Control Release, 2004, 96(1):135-148.
    [17] Botella P, Abasolo I, Fern ndez Y, et al. Surface-modified silica nanoparticles for tumor-targeted delivery of camptothecin and its biological evaluation[J].J Control Release,2011,156(2):246-257.
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Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study

doi: 10.3969/j.issn.1006-0111.2016.02.013
  • 1. No.98 Hospital of PLA, Huzhou 313000, China
  • 2. School of Medicine, Jiaxing College, Jiaxing 310014, China
  • Received Date: 2015-03-09
  • Rev Recd Date: 2016-01-12

Abstract: Objective To prepare a novel drug delivery system camptothecin loaded nanogel(CPT-PPO gel), and investigate its contents, physical and chemical properties and in vitro transdermal permeability. Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems(CPT-PLGA-PAMAM, CPT-PP), in which the Poly lactic-co-glycolic acid(PLGA) was used to load camptothecin as the nucleus and the polyamidoamine(PAMAM) G3.0 was wrapped in the surface of PLGA as the shell. Then the oleic acid(OA) was connected to CPT-PP to obtain the surface modified drug delivery system(CPT-PLGA-PAMAM OA, CPT-PPO). HPLC was used to determine the content of camptothecin in nanoparticles, transmission electron microscopy was applied to identify the nanoparticles morphology, and laser analyzer was used to determine the particle size. The hydroxypropyl methylcellulose(HPMC) was added as the base for the preparation of the nanogel(CPT-PPO gel) at last. The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃, the average particle size was(246.7±5.4) nm and the encapsulation efficiency was up to(78.7±6.9)%. Comparing to the normal gel,(CPT gel), the cumulative penetration amount and the retention amount in the skin of the nanogels(CPT-PPO gel,CPT-PP gel) were significant higher(P<0.01), the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel(P<0.05). Conclusion After modified by OA, CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.

WANG Xiang, ZHANG Liangyu, DING Baoyue, CHEN Yang. Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 148-152. doi: 10.3969/j.issn.1006-0111.2016.02.013
Citation: WANG Xiang, ZHANG Liangyu, DING Baoyue, CHEN Yang. Novel camptothecin loaded nanogel system: formulation optimization and in vitro transdermal permeability study[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(2): 148-152. doi: 10.3969/j.issn.1006-0111.2016.02.013
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