New Technological Approach for Glycyrrethic Acid Oral and Topical Administration

2020 ◽  
Vol 26 (6) ◽  
pp. 664-674 ◽  
Author(s):  
Cinzia Pagano ◽  
Luana Perioli ◽  
Paola Calarco ◽  
Alessandro Di Michele ◽  
Maria C. Tiralti ◽  
...  

Background: 18β- glycyrrhetinic acid (Gly) is the major bioactive component of licorice roots and rhizomes of the Glycyrrhiza glabra species. It shows many activities such as antiviral, anti-inflammatory, antioxidant, antimicrobial, and antifungal, however, its use in the health field is very limited due to the low water solubility. Methods: This paper deals with the development of a new technological approach for Gly dissolution rate enhancement. It consists of Gly intercalation (guest) in the interlamellar spaces between the inorganic spaces (host) of the anionic clays “hydrotalcites” (HTlc) to obtain hybrids MgAl-HTlc-Gly and ZnAl-HTlc-Gly. Gly can find applications in both systemic and local therapies, thus advantages of the use of the hybrids in these two fields were investigated. Results: Gly dissolution rate from hybrids in the intestinal environment, site in which it is preferentially absorbed, resulted enhanced (ZnAl-HTlc-Gly > MgAl-HTlc-Gly) compared to the crystalline form, thereby, making them suitable for oral administration as dry powder in hard capsules. : For a local therapy, bioadhesive, vaginal emulgels loaded with the hybrids were developed. These showed suitable mucoadhesive property to the vaginal mucosa, necessary to prolong the residence time in the application site. The emulgel containing ZnAl-HTlc-Gly showed a faster and higher release profile than that containing MgAl- HTlc-Gly. Conclusions: The obtained results suggest that Gly intercalation into HTlc, especially in ZnAl-HTlc, allows to enhance Gly dissolution when the hybrids are formulated both as oral or topical products.

2013 ◽  
Vol 250 ◽  
pp. 84-90 ◽  
Author(s):  
Sasiwimon Phothipanyakun ◽  
Siwaporn Suttikornchai ◽  
Manop Charoenchaitrakool

Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  


Author(s):  
Ekta Rajendra Lambole Ekta

There are some Sthanik Chikitsa (Local Therapies) in Ayurvedic Stree Rogas described by Ancient Acharyas that possess outstanding and satisfactory outcomes in the management of Stree -Rogas. Some of these local therapies show amazing results in the management of Stree Rogas. ‘These extraordinary local therapies should be highlighted and of course used in the management of Stree Rogas for the fruitful outcomes. Sthanik Chikitsa preferably includes Yonidhawan (Douche of vagina), Yoni-Pichudharan (tampoon soaked in medicated oil or liquid is placed into the vagina), Uttar -Basti (Medicated oil or decoction is pushed into the uterine cavity through vagina), Yoni -Dhupan (Fumigation of vagina, with medicated smoke),Yoni-Varti (Insertion of medicated wick into the vagina), Yoni-Puran (vaginal packing),Yoni-Lepan (vaginal painting), Yoni-Parisheka, Pinda Chikitsa etc. In the present study  local therapies are revised through ancient samhitas and these therapies are reviewed with their meanings, indications, application procedure and application site of the local therapy. The procedure of  local therapy is discussed considering aseptic precautions. Through this study it is my hopeful and truthful effort to motivate most of the vaidyas towards Sthanik Chikitsa in the management of Stree Rogas. This study with its simple and appropriate terms will definitely help the Vaidyas to reach to the depth of the concept and will subsequently prove to be helpful to give admirable and satisfactory outcomes to Vaidyas.


2016 ◽  
Vol 50 (4) ◽  
pp. 549-562 ◽  
Author(s):  
Mahapatra Anjan Kumar ◽  
Padala Narasimha Murthy ◽  
Nagampalli Haritha Sameeraja ◽  
Palei Narahari Narayan

RSC Advances ◽  
2015 ◽  
Vol 5 (4) ◽  
pp. 2592-2601 ◽  
Author(s):  
Raul-Augustin Mitran ◽  
Silviu Nastase ◽  
Cristian Matei ◽  
Daniela Berger

Chlorine ions can mediate the adsorption and enhance the dissolution release of aminoglutethimide from pristine and functionalized MCM-41 mesoporous silica.


2020 ◽  
Vol 16 (1) ◽  
pp. 54-64 ◽  
Author(s):  
Yuzhu Hu ◽  
Xiaoye Chen ◽  
Zongyuan Li ◽  
Songping Zheng ◽  
Yongzhong Cheng

Luteolin (Lut) is a natural flavonoid mainly extracted from vegetables and fruits. Lut shows great anti-tumor potential in many malignant cancers, which are hindered by poor water solubility and low bioavailability. Peritoneal metastasis is a challenge for colorectal cancer treatment, usually indicating unfavorable prognosis of patients. Methoxy poly(ethylene glycol)-poly(ε-caprolactone) micelles containing Luteolin (Lut-M) and thermosensitive Pluronic®F127 coated Lut-M (Lut-M-F127) were synthesized and applied in the local therapy of colorectal cancer. Drug release study of Lut-M-F127 and Lut-M suggested extended drug release, and the release of Lut from Lut-M-F127 was slower than Lut-M. It was also proved that Lut-M-F127 could transit from solution to gel at body temperature. Moreover, both Lut-Free and Lut-M micelles were capable of inducing tumor cell apoptosis and reducing cell viability in vitro. Our results further demonstrated the therapeutic effect of Lut-M-F127 treatment was much better than that of Lut-M treatment in vivo. Lut-M-F127 has shown strong ability to promote tumor apoptosis, suppress tumor proliferation and block tumor angiogenesis. In summary, Lut-M-F127 formulation may be a very promising treatment option for peritoneal metastasis in colorectal cancer in the future.


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