scholarly journals Self-assembling surfactant-like peptide A6K as potential delivery system for hydrophobic drugs

2015 ◽  
pp. 847 ◽  
Author(s):  
Feng Qiu ◽  
Yongzhu Chen ◽  
Chengkang Tang ◽  
Jie Zhang ◽  
Meng Gong ◽  
...  
Author(s):  
Neeraj Singh ◽  
Shweta Rai ◽  
Sankha Bhattacharya

Background: About two-third of new drugs reveal low solubility in water due to that; it becomes difficult for formulation scientists to develop oral solid dosage forms with a pharmaceutically acceptable range of therapeutic activity. In such cases, S-SMEEDS are the best carrier used universally for the delivery of hydrophobic drugs. SEDDS were also used, but due to its limitations, S-SMEDDS used widely. These are the isotropic mixtures of oils, co-solvents, and surfactants. S-SMEDDS are physically stable, easy to manufacture, easy to fill in gelatin capsules as well as improves the drug bioavailability by releasing the drug in the emulsion form to the gastrointestinal tract and make smooth absorption of the drug through the intestinal lymphatic pathway. Methods: We took on the various literature search related to our review, including the peer-reviewed research, and provided a conceptual framework to that. Standard tools are used for making the figures of the paper, and various search engines are used for the literature exploration.In this review article the author discussed the importance of S-SMEDDS, selection criteria for excipients, pseudo-ternary diagram, mechanism of action of S-SMEDDS, solidification techniques used for S-SMEDDS, Characterization of SEDDS and S-SMEDDS including Stability Evaluation of both and future prospect concluded through recent findings on S-SMEDDS on Cancer as well as a neoteric patent on S-SMEDDS Results: Many research papers discussed in this review article, from which it was found that the ternary phase diagram is the most crucial part of developing the SMEDDS. From the various research findings, it was found that the excipient selection is the essential step which decides the strong therapeutic effect of the formulation. The significant outcome related to solid-SMEDDS is less the globule size, higher would be the bioavailability. The adsorption of a solid carrier method is the most widely used method for the preparation of solid-SMEDDS. After review of many patents, it is observed that the solid-SMEDDS have a strong potential for targeting and treatment of a different type of Cancer due to their property to enhance permeation and increased bioavailability. Conclusion: S-SMEEDS are more acceptable pharmaceutically as compare to SEDDS due to various advantages over SEDDS viz stability issue is prevalent with SEDDS. A number of researchers had formulated S-SMEDDS of poorly soluble drugs and founded S-SMEDDS as prospective for the delivery of hydrophobic drugs for the treatment of Cancer. S-SMEEDS are grabbing attention, and the patentability on S-SMEDDS is unavoidable, these prove that S-SMEEDS are widely accepted carriers. These are used universally for the delivery of the hydrophilic drugs and anticancer drugs as it releases the drug to the gastrointestinal tract and enhances the systemic absorption. Abstract: Majority of active pharmaceutical ingredients (API) shows poor aqueous solubility, due to that drug delivery of the API to the systemic circulation becomes difficult as it has low bioavailability. The bioavailability of the hydrophobic drugs can be improved by the Self-emulsifying drug delivery system (SEDDS) but due to its various limitations, solid self-micro emulsifying drug delivery systems (S-SMEDDS) are used due to its advantages over SEDDS. S-SMEDDS plays a vital role in improving the low bioavailability of poorly aqueous soluble drugs. Hydrophobic drugs can be easily loaded in these systems and release the drug to the gastrointestinal tract in the form of fine emulsion results to In-situ solubilisation of the drug. In this review article the author's gives an overview of the solid SMEDSS along with the solidification techniques and an update on recent research and patents filled for Solid SMEDDS.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 744
Author(s):  
Ijeoma F. Uchegbu ◽  
Jan Breznikar ◽  
Alessandra Zaffalon ◽  
Uche Odunze ◽  
Andreas G. Schätzlein

Commercial topical ocular formulations for hydrophobic actives rely on the use of suspensions or oil in water emulsions and neither of these formulation modalities adequately promote drug penetration into ocular tissues. Using the ocular relevant hydrophobic drug, cyclosporine A (CsA), a non-irritant ocular penetration enhancer is showcased, which may be used for the formulation of hydrophobic actives. The activity of this penetration enhancer is demonstrated in a healthy rabbit model. The Molecular Envelope Technology (MET) polymer (N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan), a self-assembling, micelle-forming polymer, was used to formulate CsA into sterile filtered nanoparticulate eye drop formulations and the stability of the formulation tested. Healthy rabbits were dosed with a single dose of a MET–CsA (NM133) 0.05% formulation and ocular tissues analyzed. Optically clear NM133 formulations were prepared containing between 0.01–0.1% w/v CsA and 0.375–0.75% w/v MET polymer. NM133 0.01%, NM133 0.02% and NM133 0.05% were stable for 28 days when stored at refrigeration temperature (5–6 °C) and room temperature (16–23 °C), but there was evidence of evaporation of the formulation at 40 °C. There was no change in drug content when NM133 0.05% was stored for 387 days at 4 °C. On topical dosing to rabbits, corneal, conjunctival and scleral AUC0–24 levels were 25,780 ng.h g−1, 12,046 ng.h g−1 and 5879 ng.h g−1, respectively, with NM133 0.05%. Meanwhile, a similar dose of Restasis 0.05% yielded lower values of 4726 ng.h/g, 4813 ng.h/g and 1729 ng.h/g for the drug corneal, conjunctival and scleral levels, respectively. NM133 thus delivered up to five times more CsA to the ocular surface tissues when compared to Restasis. The MET polymer was non-irritant up to a concentration of 4% w/v. The MET polymer is a non-irritant ocular penetration enhancer that may be used to deliver hydrophobic drugs in optically clear topical ocular formulations.


2019 ◽  
Vol 55 (98) ◽  
pp. 14852-14855 ◽  
Author(s):  
Can Wu ◽  
Jing Liu ◽  
Xuan Tang ◽  
Ziran Zhai ◽  
Keming Xu ◽  
...  

A self-delivery system consisting of lonidamine and a self-assembling peptide was designed for the selective killing of phosphatase-overexpressing cancer cells.


2019 ◽  
Vol 566 ◽  
pp. 697-707 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Tao Wang ◽  
Wang Yin ◽  
Thao T.D. Tran ◽  
Hridika T Barua ◽  
...  

2015 ◽  
Vol 127 ◽  
pp. 266-273 ◽  
Author(s):  
Tatiana N. Pashirova ◽  
Svetlana S. Lukashenko ◽  
Sergey V. Zakharov ◽  
Alexandra D. Voloshina ◽  
Elena P. Zhiltsova ◽  
...  

2015 ◽  
Vol 38 (1) ◽  
pp. 23-29 ◽  
Author(s):  
Tomoaki Kurosaki ◽  
Chihiro Nakasone ◽  
Yukinobu Kodama ◽  
Kanoko Egashira ◽  
Hitomi Harasawa ◽  
...  

2015 ◽  
Vol 112 (10) ◽  
pp. 2978-2983 ◽  
Author(s):  
Tuo Wei ◽  
Chao Chen ◽  
Juan Liu ◽  
Cheng Liu ◽  
Paola Posocco ◽  
...  

Drug resistance and toxicity constitute challenging hurdles for cancer therapy. The application of nanotechnology for anticancer drug delivery is expected to address these issues and bring new hope for cancer treatment. In this context, we established an original nanomicellar drug delivery system based on an amphiphilic dendrimer (AmDM), which could generate supramolecular micelles to effectively encapsulate the anticancer drug doxorubicin (DOX) with high drug-loading capacity (>40%), thanks to the unique dendritic structure creating large void space for drug accommodation. The resulting AmDM/DOX nanomicelles were able to enhance drug potency and combat doxorubicin resistance in breast cancer models by significantly enhancing cellular uptake while considerably decreasing efflux of the drug. In addition, the AmDM/DOX nanoparticles abolished significantly the toxicity related to the free drug. Collectively, our studies demonstrate that the drug delivery system based on nanomicelles formed with the self-assembling amphiphilic dendrimer constitutes a promising and effective drug carrier in cancer therapy.


2019 ◽  
Vol 8 (13) ◽  
pp. 1900167 ◽  
Author(s):  
Franziska Koch ◽  
Katharina Ekat ◽  
David Kilian ◽  
Timm Hettich ◽  
Oliver Germershaus ◽  
...  

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