scholarly works Pharmaceutics and Industrial Pharmacy

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Medicinal Importance and Phytoconstituents of Underutilized Legumes from the Caesalpinioideae DC Subfamily
(MDPI, 2023-08) Ogunniyi, Q. A.; Ogbole, O. O.; Akin-Ajani, O. D.; Ajala, T. O.; Olorunsola, B.; Fettke, J.; Odeku, O. A.
Underutilized legumes are common crops in developing countries with superior dietarypotentials that could be useful sources of protein as well as some phytoconstituents. They are more tolerant of abiotic environmental conditions like drought than the major legumes. This makes them more adapted to harsh soil and climatic conditions, which helps to minimize the pressure brought on by climate change. However, despite their potential, underutilized legumes have been greatly overlooked compared to the major legumes due to supply constraints. Underutilized legumes in the subfamily Caesalpinioideae are better suited for use as animal feeds with little or no value as food for humans, and the extracts and infusions of the different parts of plant species in this subfamily are traditionally used for the treatment of different diseases. In addition, underutilized legumes in this subfamily contain phytoconstituents that are of pharmacological relevance, some of which have been isolated, characterized and evaluated for use in the treatment of a variety of disorders. Therefore, this review describes the medicinal activities of some selected underutilized legumes from five genera in the subfamily Caesalpinioideae as well as their phytoconstituents, which could be exploited as lead compounds for drug discovery
Talinum triangulare (Jacq.) Willd. mucilage and pectin in the formulation of ibuprofen microspheres
(Wroclaw Medical University, 2022) Akin-Ajani, O. D.; Hassan, T. M.; Odeku, O. A.
Background. Mucilage and pectin are both natural polymers with theadvantages ofavailability and bio¬degradability. Microspheres made from biodegradable polymers can break down naturally after performing their tasks.Objectives. Thestudy aimed touse mucilage and pectin from theleaves ofTalinum triangulare (Jacq.) Willd. aspolymer matrices for theformulation ofmicrospheres, with ibuprofen asthemodel drug.Materials and methods. Both polymers were examined under amicroscope and evaluated using measure¬ments ofviscosity, density, flow properties, swelling power, elemental analysis, Fourier-transform infrared spectroscopy (FTIR), and thedegree ofesterification (DE) for pectin. Themicrospheres were prepared using theionotropic gelation method and alginate:mucilage/pectin atratios of1:1 and 1:2. They were assessed for swellability, drug entrapment effectiveness and drug release profile. Results. Themucilage particles were ovoid while pectin particles were irregularly shaped. Pectin had higher particle, bulk and tapped densities than mucilage, while mucilage had ahigher swelling power and abetter flow than pectin. Talinum triangulare pectin isalow-methoxyl pectin with aDE of7.14%. TheFTIR spectra showed no interaction between thepolymers and ibuprofen. Thesurface morphology ofthemicrospheres without ibuprofen was smooth, while those with ibuprofen revealed aspongy-like mesh. Theswelling power ofthemicrospheres was higher inphosphate buffer with apH of7.2 than indistilled water. Theentrapment efficiency ranged within 39.57–60.43% w/w, with microspheres containing alginate:mucilage/pectin ratio of1:1having higher entrapment efficiency. Microspheres with polymer ataratio of1:1 provided alonger release (>2h), while microspheres with polymer blend of1:2 provided animmediate release ofibuprofen. Conclusions. Thepolymers ofT. triangulare could be used asmatrices inmicrosphere formulations.
Comparative Evaluation of the Disintegrant Properties of Starches from Three Cultivars of Dioscorea rotundata (Poir)
(University of Huddersfield Press, 2022) Akin-Ajani, O. D.; Agbomeji, O. I.; Odeku, O. A.; Ahmadu, U.
Dioscorea rotundata Poir starches from three cultivars (Lagos, Giwa, and Sule) were evaluated as exo-disintegrants (5 and 10%w/w) in paracetamol tablet formulations to determine whether the similarity in their physicochemical and material properties translates to performance in tablet formulation. The tablets were prepared by wet granulation and were evaluated for compressional properties (Heckel equation), mechanical strength (crushing strength and friability), and drug release (disintegration and dissolution times). Plastic deformation occurred in all tablets with rank order for the onset of plastic deformation Lagos>Giwa>Sule. An increase in the concentration of disintegrants in the tablets led to a decrease in mean yield pressure, total relative precompression density, and relative density at low pressure, but an increase in relative density at zero pressure. The crushing strength and disintegration times of the tablets were dependent on the disintegrants' concentration. All tablets passed the disintegration test (≤15min) with tablets containing the Sule cultivar producing the fastest disintegration (p<0.05). Tablets containing 10% of the Sule cultivar had the fastest release of paracetamol (t80=32.1min), though it failed the compendial standard for immediate release tablets (t80≤30min). Starches from the three cultivars despite their similar physicochemical and material properties exhibited different disintegrant properties and could find different applications as excipients in tablet formulations.
Intra and Extra-granular Disintegrant Properties of Modified Underutilised Red Lima Bean Starch in Paracetamol Tablet Formulation
(Universidade de São Paulo, Faculdade de Ciências Farmacêuticas, 2020) Okekunle, M. O.; |Akin-Ajani, O. D.; Ekpukpon, B. L.; Odeku, O. A.; Olu-Owolabi, B. I.; Adebowale, K.O
Red lima bean (Phaseolus lunatus Linn) Family Fabaceae, has been modified by succinylation and annealing, and used as intra- and extra-granular disintegrants at concentrations of 5 and 10 %w/w in paracetamol tablet formulation in comparison with corn starch BP. The starches were characterised using FT-IR spectroscopy, SEM, proximate analysis, physicochemical and functional properties. FT-IR spectrometry revealed characteristic peaks at 1575.53 and 1713.99 cm-1 for the succinylated starch while the annealed showed no significant difference from the native starch. Modifications did not alter the ovoid shape of the native starch but reduced the particle size. Succinylation improved water absorption capacity, solubility and swelling of lima bean starch but annealing reduced the parameters. Tablets with disintegrants of lima bean starches generally had higher crushing strengths and lower friability than tablets with corn starch. Modifications reduced the disintegration time of the tablets when the starcheswere incorporated intra-granularly, which suggested particle-particle bond interruption and destruction of hydrogen bonds as mechanism of disintegration. Tablets containing 10 %w/w succinylated red lima bean starch incorporated intra-granularly had the highest disintegration efficiency ratio, DER, indicating a great balance between mechanical and disintegration properties. Modified red lima bean starches incorporated intra-granularly into paracetamol ablets led to faster disintegration and could efficiently substitute corn starch as disintegrant.
Intra and Extra-granular Disintegrant Properties of Modified Underutilised Red Lima Bean Starch in Paracetamol Tablet
(International Pharmaceutical Excipients Council (IPEC), 2020-06) Akin-Ajani, O. D.; Odeku, O. A.; Olumakinde-Oni, O
Binary mixtures of microcrystalline cellulose MCC (A), and lactose (L) in ratios at 75:25, 50:50, and 25:75% respectively were prepared. The binary mixtures were subjected to microscopical analysis and density measurements. The mechanical properties of paracetamol tablets formulated with the above excipients were assessed for tensile strength, bonding capacity (using the Ryshkewitch-Duckworth relation) and friability, while drug release properties were assessed for disintegration and dissolution times. The dissolution profiles were fitted into dissolution model equations to determine release mechanism and similarity of release. Microscopic analysis showed that the lactose particles were large, crystalline, and acicular in shape whereas the MCC particles were smaller and irregularly shaped. The binary mixtures had particle shape and sizes in between the parent compounds. The particle size of A25:L75 however, was larger than that of the proprietary brand, Microcelac®. Bulk and tapped densities increased with increasing amounts of MCC in the binary mixtures while particle density had an inverse relationship. Tablets containing A75:L25 had the highest tensile strength and bonding capacity and lowest friability in comparison to other binary mixtures and Microcelac®. However, tablets containing A75:L25 did not show superiority to Microcelac® in terms of paracetamol release. Its release, however, followed the Korsmeyer-Peppas model indicating a super case II transport mechanism. Only comparisons of tablet combinations of Lactose: A25:L75 and MCC: A50:L50 had a similarity factor, f2 >50. Tablets made of A75:L25 exhibited the highest mechanical and release properties of the binary mixtures, as directly compressible excipient in comparison to the parent compounds and Microcelac®. This mixture, A75:L25 therefore, could be developed for commercial use in tablet formulations.
Evaluation of the mechanical and release properties of lactose and microcrystalline cellulose and their binary mixtures as directly compressible excipients in paracetamol tablets
(International Pharmaceutical Excipients Council (IPEC), 2020-06) Akin-Ajani, O. D.; Odeku, O. A.; Olumakinde-Oni, O
Binary mixtures of microcrystalline cellulose MCC (A), and lactose (L) in ratios at 75:25, 50:50, and 25:75% respectively were prepared. The binary mixtures were subjected to microscopical analysis and density measurements. The mechanical properties of paracetamol tablets formulated with the above excipients were assessed for tensile strength, bonding capacity (using the Ryshkewitch-Duckworth relation) and friability, while drug release properties were assessed for disintegration and dissolution times. The dissolution profiles were fitted into dissolution model equations to determine release mechanism and similarity of release. Microscopic analysis showed that the lactose particles were large, crystalline, and acicular in shape whereas the MCC particles were smaller and irregularly shaped. The binary mixtures had particle shape and sizes in between the parent compounds. The particle size of A25:L75 however, was larger than that of the proprietary brand, Microcelac®. Bulk and tapped densities increased with increasing amounts of MCC in the binary mixtures while particle density had an inverse relationship. Tablets containing A75:L25 had the highest tensile strength and bonding capacity and lowest friability in comparison to other binary mixtures and Microcelac®. However, tablets containing A75:L25 did not show superiority to Microcelac® in terms of paracetamol release. Its release, however, followed the Korsmeyer-Peppas model indicating a super case II transport mechanism. Only comparisons of tablet combinations of Lactose: A25:L75 and MCC: A50:L50 had a similarity factor, f2 >50. Tablets made of A75:L25 exhibited the highest mechanical and release properties of the binary mixtures, as directly compressible excipient in comparison to the parent compounds and Microcelac®. This mixture, A75:L25 therefore, could be developed for commercial use in tablet formulations.
Formulation and Antimicrobial Evaluation of Isopropyl Hand Sanitizer using Co-processed Excipients
(African Journals OnLine, 2020-02) Akin-Ajani, O. D.; Odeku, O. A.; Olumakinde-Oni, O
Background: In response to the Ebola virus outbreak in West Africa in the year 2014, which caused the Ebola haemorrhagic fever, the WHO alcohol-based hand rub formulation was adopted in addition to regular hand washing to prevent the spread. However, other formulation factors rather than alcohol concentration alone can greatly influence the overall antimicrobial efficacy of hand disinfectants. Objective: To formulate an antimicrobial hand sanitizer using co-processed carriers. Methodology: Carbopol (F), HPMC (G) and co-processed forms of both polymers in batches- 1:1(A), 1:2(B), 1:4(C), 2:1(D) and 4:1(E) respectively were used. The polymers were characterized, and used as carriers in formulating hand sanitizers (A to G). The formulated hand sanitizers were evaluated for physical appearance, pH, clarity, viscosity, drying time and antimicrobial activity, in comparison to a commercially available hand sanitizer (CAHS). Results: Co-processing significantly (p0.05) improved both hydration capacity of carbopol and viscosity of HPMC. The physical appearance, pH and opacity were maintained throughout the study. All the formulations showed dilatant rheological behaviour while the CAHS exhibited plastic flow. The drying times for the formulated hand sanitizers were comparable to CAHS but longer than isopropyl alcohol implying prolonged action at application site. The antimicrobial activity of the formulations was of the rank order isopropyl alcohol>B>F>CAHS>D>E>C>G>A. Conclusion: Co-processing of excipients improved the pharmaceutical properties of the hand sanitizers with antimicrobial activity that was comparable to CAHS but lower than isopropyl alcohol. The hand sanitizer formulated with polymer batch B, demonstrated optimum antimicrobial and pharmaceutical properties and may be developed for commercial use.
Application of the Gurnham equation in characterizing the compressibility of fonio and sweet potato starches and their paracetamol tablet formulations
(Nigeria Association of Pharmacists in Academia, 2018-02) Akin-Ajani, O. D.; Itiola, O. A.; Odeku, O. A.
Background: A number of empirical relationships have been proposed to describe the compaction of pharmaceutical materials, among them are the Heckel, Kawakita and Gurnham equations. Objective: To characterize the compressibility of fonio, sweet potato and corn starches and their paracetamol formulations using the Gurnham and Kawakita equations, and to determine the complementarity of these equations. Materials and Methods: Starches were extracted from fonio (Digitaria exilis) grains and sweet potato (Ipomea batatas) tubers and modified by acid hydrolysis for 96 h. Paracetamol formulations containing 2.5–10.0 %w/w starch binders were prepared by wet granulation. Packing and compaction properties of native and modified starches and their formulations were determined using tapping procedures. The data obtained was analyzed using the Gurnham and Kawakita equations. Results: The ranking for Gurnham compressibility, c, for the starches was sweet potatocornfonio, which was inversely related to the ranking for Kawakita maximum volume reduction, a and angle of internal flow, θ. There was no clear-cut pattern in the Gurnham compressibility of paracetamol formulation probably due to its multicomponent nature. There was correlation between c, a and θ for all the starches with the modified starches exhibiting higher compressibility than native starches. There appeared to be no correlation between c and Kawakita compressibility index, b. Conclusion: The Gurnham equation appeared useful in characterising compressibility in single component systems and could be used along with Kawakita functions, to gain a better understanding of the deformation of powdered materials under pressure.
Evaluation of freeze-dried pregelatinized Chinese yam (Dioscorea oppositifolia) starch as a polymer in floating gastroretenive metformin microbeads.
(2010) Okunlola, A.; Patel, R. P.; Odeku, O. A.
Pregelatinized Chinese yam (Dioscorea oppositifolia) starch has been evaluated as a polymer for the formulation of floating gastroretentive beads for the controlled delivery of metformin hydrochloride. Floating microbeads were prepared by the ionotropic gelation method using a blend of modified Chinese yam starch and sodium alginate at different ratios. Sodium bicarbonate was added as a gas-generating agent. The floating microbeads were characterized by SEM, DSC, FTIR analyses and the drug entrapment efficiency and floating ability was evaluated. Drug release was investigated using in vitro dissolution test and the results were fitted to various kinetic models to determine the mechanism(s) of release. Spherical, discrete and free flowing microbeads were obtained from the modified starch-alginate blends. Minimum lag time (< 20 s) was observed for the floating microbeads containing starch and buoyancy was maintained for 12 h. The release of MET from the floating microbeads appeared to be controlled by varying the starch to alginate polymer ratio. In general, the formulations followed diffusion and erosion mechanisms of drug release. The results suggest that modified Chinese yam starch-sodium alginate blend can be useful for the formulation of floating gastroretentive system for metformin hydrochloride
Formulation of metronidazole tablets using hydroxypropylated white yam (dioscorea rotundata) starch as the binding agent
(IPEC-Americas Inc, 2017) Okunlola, A.; Alade, O. O.; Odeku, O. A.
White yam starch obtained from the tubers of Dioscorea rotundata Poir was modified by hydroxypropylation and used as a binding agent in a metronidazole tablet formulation and compared with corn starch BP. The quantitative effects of the novel starch binder on the mechanical (tensile strength and friability) and release properties (disintegration and dissolution times) of the metronidazole tablet was analyzed using a full 23 factorial experimental design. The individual and interaction effects of type of starch binder (X1), concentration of binder (X2) and relative density (X3) on tensile strength, friability, disintegration time and dissolution time (t90) were determined. The ranking of the coefficients was X3 > X2 > X1 on T, X1 > X3 > X2 on F and X3 > X1 > X2 on DT and t90 (time for 90% drug release) indicating that the formulation variables influence the properties of metronidazole tablets to varying degrees. This indicates that the type and concentration of starch binder as well as the compression pressure employed in table formulation need to be carefully selected to obtain tablets with the desired mechanical and drug release properties. Hydroxypropyl white yam starch could be more useful as a binder especially when tablets require high mechanical strength and faster drug release are desired.

scholarly works Pharmaceutics and Industrial Pharmacy

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