Enhancement of Aqueous Solubility and Oral Bioavailability of Nelfinavir by Complexation with β- Cyclodextrin

Purpose: To determine if complexation with β- cyclodextrin (β-CD) increases water solubility and subsequent bioavailability of nelfinavir mesylate (NM).Methods: Complexation of NM with β-CD in 1:1.5 molar ratio was carried out by solvent evaporation, freeze-drying and kneading methods. The complexes were characterized by Fourier transform infrared spectroscopy (FTIR). The in vitro solubility of the pure drug as well as that of the complexes was evaluated using USP type 2 apparatus. One of the drug complexes was also evaluated in vivo using Wistar rats to determine its pharmacokinetic profile.Results: Freeze-dried NM-βCD complex was selected for in vivo studies based on its free flowing property and superior texture. The complexes prepared by the three methods all showed largely similar dissolution rate. The in vivo pharmacokinetic study of the freeze-dried complex in male Wistar rats showed significant increase in Cmax, tmax and AUC (p ≤ 0.05) compared to those of the plain drug.Conclusion: These findings suggest that complexation of NM with β-CD is an effective and promising approach to increasing the oral bioavailability of NM

Regulatory Aspects of Pharmaceuticals’ Exports in Gulf Cooperation Council Countries

The Gulf cooperation council (GCC) region is considered as “Emerging market” for pharmaceutical export and bilateral trade. The understanding of the regulatory requirements of this region can be beneficial for pharmaceutical export. Some incidents of the year 2008-09, like recession or economic slowdown in highly well-off and regulated market of the EU and US, raised the demand for alternate destinations for business. The regulations of Gulf countries are encouraging the import of quality generic products, which can be good news to the Indian drug manufacturers

Development and evaluation of sunscreen creams containing morin-encapsulated nanoparticles for enhanced UV radiation protection and antioxidant activity

Pallavi Krishna Shetty,1 Venkatesh Venuvanka,1 Hitesh Vitthal Jagani,1 Gejjalagere Honnappa Chethan,1 Virendra S Ligade,1 Prashant B Musmade,1 Usha Y Nayak,1 Meka Sreenivasa Reddy,1 Guruprasad Kalthur,2 Nayanabhirama Udupa,1 Chamallamudi Mallikarjuna Rao,1 Srinivas Mutalik1 1Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, 2Division of Clinical Embryology, Kasturba Medical College, Manipal University, Manipal, Karnataka, India Abstract: The objective of present work was to develop novel sunscreen creams containing polymeric nanoparticles (NPs) of morin. Polymeric NPs containing morin were prepared and optimized. The creams containing morin NPs were also prepared and evaluated. Optimized NPs exhibited particle size of 90.6 nm and zeta potential of -31 mV. The entrapment efficiency of morin, within the polymeric NPs, was found to be low (12.27%). Fourier transformed infrared spectroscopy and differential scanning calorimetry studies revealed no interaction between morin and excipients. Transmission electron microscopy and atomic force microscopy revealed that the NPs were spherical in shape with approximately 100 nm diameter. Optimized NPs showed excellent in vitro free radical scavenging activity. Skin permeation and deposition of morin from its NPs was higher than its plain form. Different sunscreen creams (SC1–SC8) were formulated by incorporating morin NPs along with nano zinc oxide and nano titanium dioxide. SC5 and SC8 creams showed excellent sun protection factor values (≈40). In vitro and in vivo skin permeation studies of sunscreen creams containing morin NPs indicated excellent deposition of morin within the skin. Morin NPs and optimized cream formulations (SC5 and SC8) did not exhibit cytotoxicity in Vero and HaCaT cells. Optimized sunscreen creams showed excellent dermal safety. SC5 and SC8 creams demonstrated exceptional in vivo antioxidant effect (estimation of catalase, superoxide dismutase, and glutathione) in UV radiation-exposed rats. The optimized sunscreen creams confirmed outstanding UV radiation protection as well as antioxidant properties. Keywords: nanoparticles, skin permeation, sunscreen, morin, sun protection factor&nbsp