scholarly journals Evaluation of Physicochemical Properties, Skin Permeation and Accumulation Profiles of Ketorolac Fatty Ester Prodrugs

2007 ◽  
Vol 30 (11) ◽  
pp. 2211-2216 ◽  
Author(s):  
Krishna Hari Bhandari ◽  
Madhuri Newa ◽  
Sung II Yoon ◽  
Jung Sun Kim ◽  
Ki Young Jang ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Skin Permeation ◽  
Fatty Ester ◽  
Ester Prodrugs

Synthesis, physicochemical properties and antiviral activities of ester prodrugs of ganciclovir

2005 ◽  
Vol 305 (1-2) ◽  
pp. 75-89 ◽  
Author(s):  
Kunal Patel ◽  
Shrija Trivedi ◽  
Shuanghui Luo ◽  
Xiaodong Zhu ◽  
Dhananjay Pal ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Antiviral Activities ◽  
Ester Prodrugs

Synthesis, stereoselective enzymatic hydrolysis, and skin permeation of diastereomeric propranolol ester prodrugs

1999 ◽  
Vol 88 (5) ◽  
pp. 544-550 ◽  
Author(s):  
Chandrasekhar Udata ◽  
Giridhar Tirucherai ◽  
Ashim K. Mitra
Keyword(s):  
Enzymatic Hydrolysis ◽  
Skin Permeation ◽  
Ester Prodrugs

scholarly journals Phenylethyl Resorcinol Loaded in Liposomal Cream Formulation for Cosmeceutical Application

2020 ◽  
pp. 64-76 ◽  
Author(s):  
Panithi Raknam ◽  
Sirirat Pinsuwan ◽  
Thanaporn Amnuaikit
Keyword(s):  
Physicochemical Properties ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Ethanol Injection ◽  
Superior Result ◽  
Cream Formulation ◽  
Liposome Formulation ◽  
Physicochemical Stability ◽  
Hacat Keratinocyte

Phenylethyl Resorcinol (PR) is a cosmeceutical skin lightening agent and the purpose of this study was to enhance its stability by using liposomal cream formulation which increases local efficacy and safety. Liposome formulation was prepared by modified ethanol injection method, and it contained soy phosphatidyl choline (SPC), cholesterol (CHO), Tween 80 (TW80) and deoxycholic acid (DA) mixed with 2% PR. The physicochemical properties, skin permeation as well as cellular study were evaluated in order to obtain the optimized formulation. The optimized liposome formulation composed of SPC:TW80:DA (84:16:2.5) and exhibited vesicle size, polydispersity index (PDI) and zeta potential of 286.4±8.04 nm, 0.317±0.03 and -39.20±3.85 mV, respectively. Entrapment efficiency (EE) of liposome formulation was 93.55±0.05%. The vesicle was spherical in shape and showed good physicochemical stability for 4 months. The skin permeation study demonstrated that liposome with a negative charge could result in a high PR skin deposition value of 1732.76±216.24 µg/cm2 after 24 h. Cellular study showed that liposome formulation could inhibit melanin content in B16 melanoma cells and enhance cell viability in HaCaT keratinocyte cells. The optimized PR liposome was incorporated in cream and investigated physicochemical properties, stability and skin permeation. Liposomal PR cream showed a good stability and a superior result than PR cream in skin permeation parameters, as well as in tyrosinase inhibition.

Ester prodrugs of a potent analgesic, morphine-6-sulfate: syntheses, spectroscopic and physicochemical properties

1998 ◽  
Vol 163 (1-2) ◽  
pp. 177-190 ◽  
Author(s):  
Detpon Preechagoon ◽  
Ian Brereton ◽  
Christine Staatz ◽  
Richard Prankerd
Keyword(s):  
Physicochemical Properties ◽  
Ester Prodrugs

scholarly journals Formulation and Evaluation of Guggul Lipid Nanovesicles for Transdermal Delivery of Aceclofenac

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Vidhu Aeri
Keyword(s):  
Physicochemical Properties ◽  
Water Solubility ◽  
Skin Permeation ◽  
Stability Study ◽  
New Drugs ◽  
Systemic Absorption ◽  
Accelerated Stability ◽  
Planar Molecule ◽  
Higher Temperature ◽  
Dicetyl Phosphate

Context. Most new drugs have low water solubility and liposome is an important formulation to administer such drugs; however, it is quite unstable and has negligible systemic absorption.Objective. Aceclofenac nanovesicles were made using guggul lipid for formulating stable transdermal formulation.Materials and Methods. Guggul lipid was formulated into vesicles along with cholesterol and dicetyl phosphate using film hydration method. The formulations were analyzed for physicochemical properties and stability. Then its skin permeation and anti-inflammatory activity were determined.Results. Both categories of vesicles (PC and GL) showed optimum physicochemical properties; however, accelerated stability study showed considerable differences. GL-1 was appreciably stable for over 6 months at 4°C. Corresponding gels (PCG-1 and GLG-1) showedCmaxvalues at 4.98 and 7.32 μg/mL along with theTmaxvalues at 4 and 8 hours, respectively. GLG-1 inhibited edema production by 90.81% in 6 hours.Discussion. PC liposomes are unstable at higher temperature and upon longer storage. The formulation with higher lipid content (GL-1) showed good drug retention after 24 hours and appreciable stability both at higher temperature and for longer duration. Guggul lipid being a planar molecule might be stacked in vesicle wall with cholesterol.Conclusion. The composition of the nanovesicle played an important role in stability and drug permeation. Guggul lipid is suitable for producing stable vesicles.

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