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The characteristics of intestinal model fluids were investigated at conditions which simulate the passage from the middle to the end of the duodenum. The formation and decay of liposomes and micelles in model bile fluids were studied, because of their role as an intermediate host for the resolution and uptake of hydrophobic drugs (BCS classes II, IV). The conditions, which may influence the formation of these nanoparticulate intermediates were studied, i.e., the lipid composition of the bile, the preparation method, the time of the passage through the modelled duodenum segment and the concentration, which results from the variable dilution of the bile by mixing with the transfer medium representing the fluid arriving from the stomach. The variation of the lecithin entity revealed an equivalence of egg-lecithin of a high purity (99%) with its main component 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine POPC, while 1,2-di-oleoyl-sn-glycero-3-phosphocholine DOPC resulted in a slight delay of the micelle-liposome conversion. The FeSSIF preparation method was best with the sequential-film method, while the bile-film method yielded comparable results; the shake method showed a slightly different kinetics of the nanoparticle conversion. The time and concentration dependence of the formation and decay of lipidic nanoparticles indicates that these strongly depend on the passage time (speed) and bile dilution rate. The corresponding physiological conditions in healthy persons may vary in vivo individually and due to diseases. The studied conditions cover typical physiological conditions, which should be taken into consideration in the exploration of in vitro tests of formulations of hydrophobic drugs. Practical applications:The results can be applied to improve formulation development and testing methods for difficult drugs belonging to the BCS classes 2 and 4. The main analytical method, dynamic light scattering, is available in well-equipped pharmaceutical labs. It is supported by additional investigation with neutron scattering. This is a key for a development of drug formulations yielding a sufficient bioavailability of hydrophobic drugs.

Pectin is a high molecular weight polymer which is present in virtually all plants where it contributes to the cell structure. Pectin is a high valuable food ingredient widely used as a gelling agent and thickening agent with limited use in the pharmaceutical industry. The objective of this study is to evaluate the suspending properties of pectin from watermelon rind. Tragacanth was used as a standard suspending agent to which the suspending properties of pectin from watermelon rinds were compared with. The extracted pectin was subjected to phytochemical and physiochemical characterization for its safety and suitability to use as a suspending agent. Paracetamol suspensions were formulated using tragacanth concentrations of 0.5% w/v, 1% w/v, and 2% w/v and compared with paracetamol suspensions containing the same concentrations of watermelon pectin. The suspensions were all tested for their pH, sedimentation rate, sedimentation volume, flow rate, and ease of redispersibility over a period of 4 weeks. At the end of the 4-week period, all formulated suspensions had no changes in their pH values. Suspensions containing the extracted pectin had a lower rate of sedimentation and ease of redispersibility compared to that of tragacanth. In addition, their sedimentation volumes as well as flow rates were comparable to that of the tragacanth formulations. Ultimately, pectin from watermelon rind can serve as a suitable alternative to tragacanth in formulation of pharmaceutical suspensions.

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The study sought to formulate and evaluate suppositories using a locally produced brand of alum (Aw) obtained from bauxite waste generated at Awaso bauxite mine in the Western-North region of Ghana, for use in the treatment of hemorrhoids. The suppositories were formulated using shea butter modified, respectively, with amounts of beeswax and theobroma oil. In another development, theobroma oil was modified with different concentrations of beeswax. Drug-base interactions were investigated using attenuated total reflection-Fourier transform infrared (ATR-FTIR) spectroscopy. The suppositories were prepared using the hot melt and trituration methods. Quality control checks were carried out on the formulations. The evaluated parameters included physical characteristics (texture, presence or absence of entrapped air, and contraction holes), weight uniformity, disintegration time, drug content, and in vitro release profile of the alum from the formulated suppositories. An in vivo analysis was carried out on the most suitable formulation to ascertain its efficacy on inflamed tissues using croton oil-induced rectal inflammation in a rat model. A critical examination of the ATR-FTIR spectra revealed no drug-base interactions. The suppository formulations passed all Pharmacopoeia stated tests. The in vivo study revealed the use of suppositories ameliorated the croton oil-induced hemorrhoid in the rectoanal region of the rats.