Purpose: A curcumin-docetaxel co-loaded nanosuspension with increased anti-breast cancer activity was developed. Curcumin is a potential anticancer agent with p-glycoprotein (p-gp) inhibiting activity may be co-administered with docetaxel as a nanosuspension to enhance its anticancer effect by increasing the oral bioavailability and decreasing drug efflux. Methods: Nanosuspensions of curcumin and docetaxel were prepared by precipitation-homozenisation technique and evaluated for particle size, polydispersity, zeta potential and drug release. The in vitro MTT assay was conducted using MCF-7 for anti-breast cancer activity. The in vivo biodistribution by radiolabeling and tumor inhibition study was conducted in mice. Results: Homogenous nanosuspensions of 80 ± 20 nm were obtained with increased solubility. The drugs as nanosuspensions showed higher cytotoxicity on MCF-7 cell line compared to their suspensions due to the increased in vitro cellular uptake. Due to this increased solubility, sensitization of tumor cells and inhibition of p-gp the in-vivo results showed greater tumor inhibition rate of up to 70% in MCF-7 treated mice. Histopathological results showed higher apoptotic activity and reduced level of angiogenesis. Conclusions: The in vitro and in vivo study of the nanosuspensions has shown that Co-administration of Curcumin as a p-gp inhibitor with docetaxel may have the potential to increase the anti-breast cancer efficacy of both drugs.

Starch has emerged as a new attractive biopolymer for use in pharmaceutical applications, owing to its distinctive physical, chemical and functional properties. This biopolymer has several potential advantages: it is biocompatible, low cost, non-toxic and easily isolated from plant sources. In the pharmaceutical field, starch is used as a raw material for developing various drug delivery platforms. Generally, cassava starch (tapioca) is obtained from the swollen roots of the perennial shrub Manihot esculenta and it contains a low amount of amylose in contrast to other varieties of starches. Because of this reason, cassava starch exhibits various prime benefits, including a low gelatinization temperature, higher swelling power and a relatively high viscosity paste, making it a preferable excipient for pharmaceutical applications. However, cassava starches in their native form are not effective for many applications because of their inefficiency in handling various processing requirements like high temperature and diverse pH. Their applicability can be enhanced by starch modification. These functional starches have demonstrated outstanding prospects as primary excipients in many pharmaceutical formulations. In this article, we discuss the potential application of cassava starches in the pharmaceutical and biomedical fields, along with the toxicity assessment of modified cassava starches.

The aim of this study was to formulate and evaluate microencapsulated controlled release preparations of zidovudine using ethyl cellulose as the retardant material with high entrapment efficiency and extended release. Microspheres were prepared by water-in-oil-in-oil (w/o/o) double emulsion solvent diffusion method. A mixed solvent system (MSS) consisting of acetonitrile and dichloromethane in a 1:1 ratio and light liquid paraffin were chosen as primary and secondary oil phases, respectively. Span 80 was used as the surfactant for stabilizing the secondary oil phase. The prepared microspheres were white, free flowing and spherical in shape and characterized by drug loading, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in vitro release studies were performed using PH 7.4 phosphate buffer. The drug loaded microspheres showed 41–55% of entrapment and release was extended up to 18–20 h. The infrared spectra and DSC and DTA thermograms showed stable character of zidovudine in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. Data obtained from in vitro release were fitted to various kinetic models and high correlation was obtained in the Higuchi model. The drug release was found to be diffusion controlled.

NeuroAIDS (Neuro Acquired Immunodeficiency Syndrome) or HIV (Human Immunodeficiency Virus) associated neuronal abnormality is continuing to be a significant health issue among AIDS patients even under the treatment of combined antiretroviral therapy (cART). Injury and damage to neurons of the brain are the prime causes of neuroAIDS, which happens due to the ingress of HIV by direct permeation across the blood-brain barrier (BBB) or else via peripherally infected macrophage into the central nervous system (CNS). The BBB performs as a stringent barricade for the delivery of therapeutics drugs. The intranasal route of drug administration exhibits as a non-invasive technique to bypass the BBB for the delivery of antiretroviral drugs and other active pharmaceutical ingredients inside the brain and CNS. This method is fruitful for the drugs that are unable to invade the BBB to show its action in the CNS and thus erase the demand of systemic delivery and thereby shrink systemic side effects. Drug delivery from the nose to the brain/CNS takes very less time through both olfactory and trigeminal nerves. Intranasal delivery does not require the involvement of any receptor as it occurs by an extracellular route. Nose to brain delivery also involves nasal associated lymphatic tissues (NALT) and deep cervical lymph nodes. However, very little research has been done to explore the utility of nose to brain delivery of antiretroviral drugs in the treatment of neuroAIDS. This review focuses on the potential of nasal route for the effective delivery of antiretroviral nanoformulations directly from nose to the brain.

The aim of our study was to investigate the enhancing effect of several essential oils in the percutaneous absorption of trazodone hydrochloride (TZN). For this purpose, fennel oil, eucalyptus oil, citronella oil, and mentha oil were applied on the skin membrane in three different ways: included in the transdermal device, as a pretreatment, or both. To investigate the effect of penetration enhancers used in this study on the percutaneous absorption of TZN through mouse epidermis, Keshary-Chien diffusion cells were employed. The receptor phase was constantly stirring saline phosphate buffer of pH 7.4 at 37 ± 1°C. Results showed that pretreatment of skin with essential oils increases the flux values of TZN compared with the values obtained when the same essential oils were included in the transdermal devices. The percutaneous penetration flux for TZN was increased with skin pretreatment by 10% essential oils in the following order: fennel oil > eucalyptus oil > citronella oil > mentha oil. The amount of TZN retained in the skin after pretreatment with essential oils was found to be very similar in all cases and much higher than in the experiments without skin pretreatment.

The drug with poor oral bioavailability necessitates the development of novel carrier for efficient drug delivery. This paper reports the rutin–phospholipid complex in polymer matrix for sustained delivery of rutin via the skin for the treatment of acute and chronic inflammatory diseases. Rutin in phospholipid complex (RNPs) are better soluble and permeable than the free rutin. The RNPs-loaded polymeric matrix patch with moderate adhesiveness was developed for convenient means of long term drug application on the skin. The patch was analysed for physicochemical properties, ex vivo skin permeability and in vivo efficacy in rat paw oedema model. The skin targeting efficacy was analysed by CLSM study. Optimized formulation (F2) showed 31 ± 2.32% and 26.56 ± 5.52% skin permeation at 24 h across excised rat skin and human cadaver skin, respectively. The sustained anti-inflammatory effect of the patch formulation in rat paw oedema model confirmed its unique in vivo efficacy over the conventional diclofenac gel. The CLSM study confirmed the localization of RNPs in the dermis for sustained anti-inflammatory effect. Our results suggest that the developed patch has a potential for long term site specific delivery of rutin in arthritic patients.