M. Tech. Pharmaceutical Sciences / Following the discovery of an active pharmaceutical ingredient, attempts were made to improve its delivery to the site of action and thereby its effectiveness. Insulin and other therapeutic proteins are administered almost exclusively parenterally because of their poor absorption after oral administration, but this route is associated with disadvantages including pain, discomfort and lipohypertrophy at the site of injection. A suitable absorption enhancer which could effectively improve the absorption of poorly absorbable drugs from the gastrointestinal tract would contribute to the development of an effective oral drug delivery system for these drugs. One such attempt was the formulation of the active ingredient into an appropriate dosage form for a specific route of administration to improve other properties such as manufacturability, stability and bioavailability. Formulation studies led to the development of substances called excipients, which were incorporated into dosage forms, in addition to the active pharmaceutical ingredient, to improve the properties of the final product. Aloe vera gel previously showed the ability to increase the bioavailability of vitamins and to enhance the in vitro transport of a macromolecular drug across intestinal epithelial cell monolayers. However, the effect of leaf materials from aloes, indigenous to South Africa, on drug transport across intestinal epithelia has not previously been investigated. The aim of this study is to evaluate the in vitro drug transport enhancement potential of the gel and whole leaf extract of Aloe ferox, Aloe marlothii, Aloe speciosa and compare them with that of Aloe vera across Caco-2 cell monolayers, as well as across excised rat intestinal tissues.

Thesis (M. Tech. (Biomedical Technology)) -- Central University of Technology, 2014 / The rising costs of health care, the outbreak of drug resistant organisms, health depleting lifestyles and the risky side effects of currently used drugs are world-wide problems. This has led to the search for novel drugs and drug leads. Traditional healers and other individuals across the globe possess unlimited knowledge on the healing powers of different plants that has been passed on through generations. This knowledge together with scientific investigations can lead to the eradication of most of the diseases either by treatment or prevention. Aloe ferox Mill. is one of the plants that have gained a lot of interest from the pharmaceutical industry. The plant has over 80 documented medicinal uses. These include treatment of impotence and infertility, sexually transmitted infections, arthritis, hypertension, leukaemia, bacterial and fungal infections. It is also known as a blood purifier, widely used as a laxative and anti- inflammatory agent. More research is required to discover more about A. ferox and its benefits to health as well as to investigate its potential for the development of novel drugs. The current study was focused at investigating the anti- cancer, anti- microbial antidiabetic, cytotoxic activities and phytochemical composition of leaf extracts of A. ferox. Three cancer cell lines namely: breast (MCF7), colon (HCT116) and prostate (PC3) cancer cell lines were used to investigate the anticancer activity of the extracts using the Sulforhodamine B (SRB) method. To determine the anti- diabetic activity of the plant extracts the C2C12 and Chang cell in- vitro models of glucose uptake were used. The micro- dilution technique was IV used to evaluate the antibacterial and antifungal activity of the extract. The safety of these extracts against normal human foetal lung fibroblasts (W138), Chang and C2C12 cells was done by through the SRB and the MTT methods. To determine the phytochemical profile of A. ferox the DPPH radical scavenging and the Folin Ciocalteu methods were used to test the antioxidant activity and the total phenolic content of the different extracts respectively. Different methods were used to determine the presence of phytochemicals such as steroids, saponins, alkaloids, carbohydrates and flavonoids. LCMS was also done to detect the elemental composition of the plant extracts. According to the CSIR criteria A. ferox was inactive against the cancer cell lines used. It however exhibited antioxidant activity even at low concentrations, with an EC50 of 0.865 ± 0.783. The methanol extract showed more phenolic content than the dichloromethane and aqueous extracts at a concentration of 5mg/ml. It is believed that the antioxidant activity correlates with the phenolic content and quality of the phenols present in the plant and more assays have to be done to prove this hypothesis. Other phytochemicals found in the extract included saponins, steroids, alkaloids as well as flavonoids. Both the methanol and aqueous extracts of A. ferox caused a significant increase in glucose uptake by C2C12 cells but caused a slightly decreased uptake by the Chang cells. The plant extracts inhibited the growth of Staphylococcus epidermidis, Streptococcus pneumonia, Escherichia coli and Candida albicans at a concentration of 15mg/ml extract. Candida tropicalis and Escherichia faecalis were resistant to A. ferox extracts. Finally the extracts showed no toxic activity against the normal foetal lung fibroblasts, Chang and C2C12 cells validating the safety of this plant for human use. V The results in conjunction with literature findings show A. ferox to be a promising source of drugs and therapeutic agents. Due to the fact that traditional healers already rely on it as treatment for different ailments, it is important that the safety of the plant for use has been validated though other studies and clinical trial still need to be done to fully confirm this. All the information gathered also showed this plant to be of great benefit against major health problems, responsible for millions of deaths each year such as cancer, cardiovascular and inflammatory diseases, and diabetes. There is however still a great need for more investigation to be done on this plant against a vast majority of organisms and diseases so as to fully benefit from it.