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A co-loaded super deformable liposome targeting anti-squamous cell carcinoma of the skin and its preparation method and application

A technology of deformed liposome and squamous cell carcinoma, which is applied in the field of medicine, can solve the problems of reduced photodynamic therapy effect, low permeability, and weak penetration depth of photodynamic light source, so as to avoid premature drug release and reduce toxicity. Side Effects, Achieving Therapeutic Index Effects

Active Publication Date: 2020-06-23
SHANGHAI DERMATOLOGY HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ALA-PDT treatment has bottlenecks such as weak penetration depth of photodynamic light source, low skin permeability of ALA, skin toxicity caused by non-specific absorption of photosensitizer, and reduced photodynamic therapy effect caused by hypoxia at the tumor site.

Method used

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  • A co-loaded super deformable liposome targeting anti-squamous cell carcinoma of the skin and its preparation method and application
  • A co-loaded super deformable liposome targeting anti-squamous cell carcinoma of the skin and its preparation method and application
  • A co-loaded super deformable liposome targeting anti-squamous cell carcinoma of the skin and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Preparation and performance characterization of co-loaded super deformable liposome [rS3-PA-ProTS / (ALA / HIF-1α siRNA)] targeting anti-squamous cell carcinoma of the skin

[0044] 1. Modified super deformable liposomes (protransfersomes, ProTS) with rS3-PA to construct a nano-targeted drug delivery system co-loading ALA and HIF-1α siRNA [rS3-PA-ProTS / (ALA / HIF-1α siRNA)] , the specific preparation method is as follows:

[0045] (1) Synthesis of HIF-1α siRNA: Human HIF-1α siRNA (sequence: 5'-CUGAUGACCAGCAACUUGAtt-3' ) and control HIF-1α siRNA.

[0046] (2) Synthesize rS3-PA according to the literature [Borghouts C, et al. JAKSTAT, 2012; 1(1):44-54], the sequence is: N-VRH SAL HMA VGP LSW PAR VS-C.

[0047] (3) Synthesis of DSPE modified rS3-PA: via distearoylphosphatidylethanolamine-polyethylene glycol 2000 -N-Hydroxysuccinimide (DSPE-PEG 2000 -NHS) reacts with the amino group of rS3-PA to produce a stable amide bond to obtain DSPE-PEG 2000 -rS3-PA. Specific...

Embodiment 2

[0089] Example 2 Preparation of co-loaded super deformable liposomes [rS3-PA-ProTS / (ALA / HIF-1α siRNA)] targeting anti-squamous cell carcinoma of the skin

[0090] Synthesis of DSPE modified rS3-PA: Precisely weigh appropriate amount of rS3-PA and DSPE-PEG 2000 -NHS (molar ratio rS3-PA:DSPE-PEG 2000 -NHS=1:2), respectively dissolved in DMF, mixed the two, stirred at room temperature for 24h to make it fully mixed; added triethylamine to adjust the solution to weak alkalinity (pH 7.0~8.0), continued the reaction at room temperature for 36h, The reaction is tracked by thin-layer chromatography until the amount of rS3-PA no longer decreases, the reaction solution is placed in a dialysis bag, dialyzed with purified water, freeze-dried, and obtained.

[0091] Preparation of rS3-PA-ProTS / (ALA / HIF-1α siRNA), accurately weigh HSPC, sodium cholate, F-68, DSPE-PEG2000 、DSPE-PEG 200 0-rS3-PA (mass ratio 4:4:4:0.1:0.1), put it into a dry and clean rotary evaporating flask, add isopropano...

Embodiment 3

[0092] Example 3 Preparation of co-loaded super deformable liposomes [rS3-PA-ProTS / (ALA / HIF-1α siRNA)] targeting anti-squamous cell carcinoma of the skin

[0093] Synthesis of DSPE modified rS3-PA: Precisely weigh appropriate amount of rS3-PA and DSPE-PEG 2000 -NHS (molar ratio rS3-PA:DSPE-PEG 2000 -NHS=1:6), respectively dissolved in DMF, mixed the two, stirred at room temperature for 24h to make it fully mixed; added triethylamine to adjust the solution to weak alkalinity (pH 7.0~8.0), and continued the reaction at room temperature for 36h, The reaction is tracked by thin-layer chromatography until the amount of rS3-PA no longer decreases, the reaction solution is placed in a dialysis bag, dialyzed with purified water, freeze-dried, and obtained.

[0094] Preparation of rS3-PA-ProTS / (ALA / HIF-1α siRNA), accurately weigh HSPC, sodium cholate, F-68, DSPE-PEG 2000 、DSPE-PEG 200 0-rS3-PA (mass ratio 2:6:6:0.1:0.1), put it into a dry and clean rotary evaporating flask, add isop...

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Abstract

The invention relates to the technical field of medicine, in particular to a targeted anti-cSCC (cutaneous squamous cell carcinoma) co-carrying super deformation liposome as well as a preparation method and application thereof. The invention aims at the bottleneck problem of the PDT (photodynamic therapy), and firstly builds pepaptamer rS3-PA mediated photosensitizers ALA (5-aminolevulinic acid) and HIF-1alphasiRNA combined co-carrying super deformation liposome; the distribution of the photosensitizers ALA on the cutaneous squamous cell carcinoma tissues / non-carcinomatous tissues is changed; through RNA (ribonucleic acid) interference, the sensitivity of the photosensitizers is improved; the PDT therapeutic index improvement is realized; meanwhile, the toxic and side effects due to non-specific absorption of the photosensitizers is reduced. The anti-cSCC effect is achieved at multiple levels of gene inhibition, PDT sensibilization, targeted medication and the like; a novel path is opened for building an anti-cSCC percutaneous targeted drug delivery system; meanwhile, the theoretical basis is also provided for the gene treatment and PDT combined use.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a co-loaded super-deformed liposome targeting anti-squamous cell carcinoma of the skin and its preparation method and application. Background technique [0002] Cutaneous squamous cell carcinoma (cSCC) is one of the most common and most harmful skin malignancies of the human head, face and genitals, accounting for about 20% of non-melanoma skin tumors. Cancer is more common. Studies have shown that some cSCC patients with specific disease risk factors are prone to recurrence, metastasis, and even death; such as lesions with a diameter ≥ 2 cm, located in the ears or red lips, facial mask areas, hands, feet, genitals, or embryonic fusion sites, Lesions with a thickness greater than 2 mm and poorly differentiated tissue or invading subcutaneous tissue (peripheral nerves, blood vessels, or lymphoid tissue). Lesions involving well-known nerves or involving nerves larger than 0.1 mm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/64A61K47/60A61K41/00A61K48/00A61K38/10A61P35/00
CPCA61K38/10A61K41/0061A61K48/005A61K2300/00
Inventor 陈中建朱全刚安多朋沈敏石磊丁佳宁孟鸽飞武喜营喻琴
Owner SHANGHAI DERMATOLOGY HOSPITAL
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