Igbinedion University Okada Journal of Pharmaceutical Sciences

Physicochemical characterization and evaluation of the suspending properties of Citrullus lanatusseed waste composite

2025-08-13T06:39:56+00:00

Background and aim: Biomaterial composite waste can be processed for application as pharmaceutical excipient. This study was aimed at assessing the suspending properties of Citrullus lanatus seed composite waste, after defatting, in the formulation of metformin suspension.
Methods: Defatted dried C. lanatus seed powder was subjected to micromeritics, water-holding and oilholding, viscosity, pH, and microscopy pre-formulation studies. Eleven batches of metformin suspensions (100 ml) were formulated using 1, 2, 4, 6 and 8% w
/ v of the composite powder, similar concentration ranges of xanthan gum, and a control batch. The pH, sedimentation volume, and re-dispersion number of the suspensions were determined.
Results: Citrullus lanatus seed yielded 56.31% composite powder having Carrs’ index < 11.32, and angle of repose < 39.05. Pre-formulation studies revealed 3.81 g H2O/ g water-holding capacity, and 2.53 g oil/g oil-holding capacity. While pH of the aqueous composite decreased with storage, viscosity increased with concentration (p < 0.05) and remains relatively stable at < 40oC. The TEM and SEM analyses of the composite-metformin blend revealed unique mesh-like and closely packed continuous sheaths. The composite suspension did not thicken on storage, and was not easily re-dispersed especially at higher concentration.
Conclusion: Citrullus lanatus seed composite showed good processing qualities, water-holding capacity and oil-holding capacity, passable thermal stability, and limited suspending properties. It demonstrated potential for optimization and for further research as emulsifier, and in combination with pharmaceutical gums as suspending agents.

Self-emulsifying properties of Moringa oleifera seed oil and Camelus homolipid (camel fat) for the delivery of 5- fluorouracil (5-fu) in the management of breast cancer

2025-08-13T06:51:56+00:00

Background and Aim: To formulate a self-emulsifying drug delivery system (SEDDS) based on Moringa seed oil (MSO) and its admixture with a homo-lipid from camel hump fat, Camelus dromedarius (CDH) for the delivery of 5-Fluorouracil for the management of breast cancer.
Method: MSO and CDH were extracted and characterised using standard methods, and utilized in the formulation of SEDDS (coded SDA1 to SDA4) loaded with 5-fluorouracil (5-FU). The properties of these were investigated with reference to isotropic test, droplet size determination, polydispersity index (PDI), zeta potential (ZP), emulsification time, absolute drug content, and percentage mortality against MCF-7 cell line. Granule formulations prepared through wet granulation technique were subjected to Carr’s and Hausner’s ratios analysis, encapsulated using hard gelatin shells, and subjected to relevant Pharmacopoeia quality control tests.
Results: MSO and CDH yielded 41 and 43% v/w, respectively with their oleic acid contents being MSO (72.5%) and CDH (39.2%). The saponification, crude fat, protein, carbohydrate, and ash values showed no significant differences from previously reported values. All formulations of 5-FU-loaded SEDDS were stable with no sign of precipitation or colour changes, gave mean emulsification times ≤ 40 minutes, and all droplet sizes were within the nano range (199 to 222.1 nm). The formulations were stable and polydisperse, as indicated by their PDI (< 0.5) and ZP (-40 mV) values. PDI, ZP and the IC50 were ranked as: SDA1≤ SDA4 ≤ SDA2 ≤ SDA3. Granules' flow parameters (p ≤ 0.05) are ranked: SDA1≤ SDA4 ≤ SDA2 ≤ SDA3, except for the flow rate of granules having a reverse ranking: SDA1≥SDA4 ≥ SDA2 ≥ SDA3. All formulations of 5-FU-loaded SEDDS capsules complied with United States Pharmacopeia requirements. SDA2 and SDA3 failed content uniformity test, which may be a direct consequence of the 5-FU SEDDS composition and the batch processing variables.
Conclusion: The Moringa seed oil and C. dromedarius homolipid were successively utilised in the formulation of SEDDS. Only SDA1 and SDA4 performances were pharmacopoeial compliant, and require further in vivo investigation and optimisation.

Comparative study of the binding strength of cellulose extracted from cassava peel and commercial polymers in cloxacillin tablet formulation

2025-08-13T06:59:00+00:00

Background and aim: This study investigated the comparative binding strength of cellulose extracted from Manihot esculenta (cassava) peel (CPC) with commercial acacia gum BP and carnauba wax BP on the mechanical strength in the formulation of Cloxacillin tablets.

Methods: Cellulose extracted from local cassava peel was subjected to phytochemical analysis. Cloxacillin granules were prepared by wet granulation using the three binders at concentrations of 2.5, 5.0, 7.5 and 10 % w/v. Micromeritic parameters of the granules, incorporating flow rate, angle of repose, bulk and tapped densities, Carr’s index and Hausner’s ratio, were determined. Physicochemical tests (hardness, weight uniformity, friability, disintegration and moisture absorption), and differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were conducted on extracted cellulose.

Results: Phytochemical analysis indicated presence of only flavonoids, alkaloids and tannins. Bulk density values were - CPC 0.725, acacia gum 0.737, carnauba wax 0.741 (g/cc³ ); tapped densities - CPC 0.777, acacia gum 0.794, carnauba wax 0.816 (g/cc³); Hausner’s ratio – CPC 1.07, acacia gum 1.08, carnauba wax 1.10; flow rate – CPC 3.33, acacia gum 2.68, carnauba wax 2.45 (g/sec). Angle of repose for all formulations were good (≤ 20^o) indicative of good flow properties. Physicochemical tests on Cloxacillin tablets showed mean values for hardness ≥ 4 kg, friability 0.446%, disintegration time 5.63 minutes. The tablets obtained from carnauba wax, however, were not satisfactory. CPC-derived tablets absorbed more moisture than those of acacia. The DSC of CPC had peak melting temperature of about 43.5^oC.

Conclusion: Study concludes that the binding strength of CPC compares favourably with that of acacia gum BP in the formulation of Cloxacillin tablets.

Assessment of disintergrant properties of Pleurotus tuberregium, corn starch and Hydroxypropyl methylcellulose in Cloxacillin trihydrate capsule formulations

2025-08-13T07:08:04+00:00

Background and aim: This research is aimed at evaluating Pleurotus tuber-regium (PTR) as a local pharmaceutical excipient and compare its disintegrant properties with standard disintegrants, corn starch BP and hydroxylpropyl methylcellulose (HPMC) BP in Cloxacillin trihydrate capsule formulation.

Methods: Micronised powder and powder prepared from the giant mushroom, P. tuber-regium (Fr) Sing, corn starch BP and HPMC powders were subjected to physicochemical tests (pH, hydration capacity, swelling capacity) and micromeritic tests. Wet granulation method with 7.5 %w/v microcrystalline cellulose as binder was used to produce Cloxacillin trihydrate granules using concentrations of 5.0, 7.5, 10.0 and 12.5 %w/w of the disintegrants. After drying the wet mass and sieving, granule bulk was lubricated, mixed and hand-filled into gelatin capsules to give Cloxacillin trihydrate 500 mg capsules. Physicochemical properties - weight uniformity, disintegration time and moisture absorption tests were evaluated.

Results: Micromeritic and powder properties of the disintegrants were comparable. At similar disintegrant concentrations, disintegration time of Cloxacillin trihydrate capsules formulated with PTR powder was less than those formulated with corn starch and HPMC. At 7.5 %w/w, disintegration time (minute) were: PTR 6.30 ± 0.23, corn starch 6.40 ± 0.15 and HPMC 8.50 ± 0.02. Disintegration time decreased with increase in disintegrant concentration. Weight variation for all formulations were within Pharmacopoeial standards of not more than ± 5% for solid dosage forms ≥ 324 mg.

Conclusion: P. tuber-regium powder as a disintegrant in Cloxacillin trihydrate capsule formulation, showed greater disintegrant ability than formulations with the standard disintegrants. Therefore, the mushroom, P. tuberregium powder could be used as a suitable substitute for corn starch BP and HPMC in Cloxacillin trihydrate capsule formulation.