Tetraacuo-bis-(N,N-dimethylacetamide-O)magnesium(II) chloride dihydrate. An option to improve magnesium effect on phosphatase stimulation and albumin binding

Background: Dermatitis is a common inflammatory skin disease that is affecting up to 25% of children and 1%-3% of adults worldwide. Paucity of exact cure for dermatitis and untoward side effects of topical immunosuppressive steroids has resulted into a great need for making use of complementary medicine to treat dermatitis. Objective: The present research work involved the development of Berberine chloride dihydrate (BCD) enthused nanovesicles i.e. ethosomes for the management of dermatitis. Method: Ethosomes were prepared by slight modification of cold method using varying concentrations of SPC (1-3%) and ethanol (10-40%) Optimized batch BCD 12 was further added to Carbopol 934P for gel formation. GEL BCD 12 was subjected to “anti-bacterial, dermatitis and skin irritation study. Result: The vesicles were in size range 142.42-398.31 nm while polydispersity index (PDI) ranges from 0.114-1.56 and for zeta potential it was from-18.8 to -39.4. Entrapment efficiency was from 46.05-88.79 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin upto 110 µm which was significantly higher than rhodamine solution (10 µm). In the anti-bacterial study, BCD loaded ethosomal gel (EG) showed maximum zone of inhibition of 18.5 mm against E. coli, 14.5 mm against P. aeruginosa and 23.0 mm against S. aureus. In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed marked decrease in amount of inflammatory cell nucleus in mice treated with BCD loaded ethosomal gel followed by 56% and 50 % increase in ear swelling and ear mass respectively in morphology study. Conventional marketed formulation showed nominal decrease in epidermal thickness, 66.67 % increase in ear thickness and 63.64 % increase in ear mass. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Conclusion: It can be concluded that ethosomal gel is not only an efficient carrier for BCD but also proves its potential for the management of dermatitis.

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Comparative Preclinical Evaluation of HER2-Targeting ABD-Fused Affibody® Molecules 177Lu-ABY-271 and 177Lu-ABY-027: Impact of DOTA Position on ABD Domain

Pharmaceutics ◽

10.3390/pharmaceutics13060839 ◽

2021 ◽

Vol 13 (6) ◽

pp. 839

Author(s):

Yongsheng Liu ◽

Anzhelika Vorobyeva ◽

Tianqi Xu ◽

Anna Orlova ◽

Annika Loftenius ◽

...

Keyword(s):

A Priori ◽

Albumin Binding ◽

Tumor Uptake ◽

Site Specific ◽

Affibody Molecules ◽

Preclinical Evaluation ◽

Renal Uptake ◽

C Terminus ◽

Minimal Modification ◽

Structure Properties

Radiolabeled Affibody-based targeting agent 177Lu-ABY-027, a fusion of an anti-HER2 Affibody molecule with albumin binding domain (ABD) site-specifically labeled at the C-terminus, has demonstrated a promising biodistribution profile in mice; binding of the construct to albumin prevents glomerular filtration and significantly reduces renal uptake. In this study, we tested the hypothesis that site-specific positioning of the chelator at helix 1 of ABD, at a maximum distance from the albumin binding site, would further increase the strength of binding to albumin and decrease the renal uptake. The new construct, ABY-271 with DOTA conjugated at the back of ABD, has been labelled with 177Lu. Targeting properties of 177Lu-ABY-271 and 177Lu-ABY-027 were compared directly. 177Lu-ABY-271 specifically accumulated in SKOV-3 xenografts in mice. The tumor uptake of 177Lu-ABY-271 exceeded uptake in any other organ 24 h and later after injection. However, the renal uptake of 177Lu-ABY-271 was two-fold higher than the uptake of 177Lu-ABY-027. Thus, the placement of chelator on helix 1 of ABD does not provide desirable reduction of renal uptake. To conclude, minimal modification of the design of Affibody molecules has a strong effect on biodistribution, which cannot be predicted a priori. This necessitates extensive structure-properties relationship studies to find an optimal design of Affibody-based targeting agents for therapy.

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18F labelled albumin binding synthons enabling PET imaging and enhanced target accumulation of biomolecules

Nuclear Medicine and Biology ◽

10.1016/s0969-8051(21)00331-0 ◽

2021 ◽

Vol 96-97 ◽

pp. S41-S42

Author(s):

Andrew Hall ◽

Alicia Corlett ◽

Mohammad Haskali

Keyword(s):

Pet Imaging ◽

Albumin Binding

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Adherence of platelets to in situ albumin-binding surfaces under flow conditions: role of surface-adsorbed albumin

Biomedical Materials ◽

10.1088/1748-6041/7/4/045007 ◽

2012 ◽

Vol 7 (4) ◽

pp. 045007 ◽

Cited By ~ 2

Author(s):

Sanjukta Guha Thakurta ◽

Robert Miller ◽

Anuradha Subramanian

Keyword(s):

Albumin Binding ◽

Flow Conditions

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Novel albumin-binding photothermal agent ICG-IBA-RGD for targeted fluorescent imaging and photothermal therapy of cancer

RSC Advances ◽

10.1039/d0ra09653a ◽

2021 ◽

Vol 11 (13) ◽

pp. 7226-7230

Author(s):

Cheng Yu ◽

Enhua Xiao ◽

Pengfei Xu ◽

Jingjing Lin ◽

Linan Hu ◽

...

Keyword(s):

Photothermal Therapy ◽

Tumor Targeting ◽

Fluorescent Imaging ◽

Albumin Binding

In this work, we present a novel photothermal agent ICG-IBA-RGD based on albumin-binding strategy for enhanced tumor targeting imaging and photothermal therapy.

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