scholarly works Pharmaceutics and Industrial Pharmacy

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Author: search.filters.author.Akin-Ajani, O. D.

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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
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    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.
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    Irvingia gabonensis (O’Rorke) Bail polymer matrix system for controlled drug delivery
    (Wroclaw Medical University, 2022-10) Patani, B. O.; Akin-Ajani, O. D.; Kumaran, A.; and Odeku, O. A
    Background. Irvingia gabonensis kernel polymer has gained attention indrug delivery systems because ofits compatibility and degradation under natural and physiological conditions. Objectives. This study aimed toevaluate Irvingia gabonensis polymer asamatrix system for thecontrolled delivery of ibuprofen incomparison toxanthan gum and hydroxypropylmethylcellulose (HPMC). Materials and methods. Irvingia gabonensis polymer was extracted using established methods and dried using theoven- and freeze-drying methods. Ibuprofen tablets were prepared bydirect compression and theeffects ofpolymer concentration (10–50%), excipients (lactose, microcrystalline cellulose and dicalcium phosphate dihydrate) and polymers (xanthan gum and HPMC) onthemechanical and drug release proper¬ties ofthetablets were evaluated. Density measurements and theHeckel and Kawakita equations were used todetermine thecompression properties ofthetablets. Friability, crushing strength and thecrushing strength–friability ratio (CSFR) were used toevaluate themechanical properties ofthetablets, while dis¬solution times were used toevaluate drug release from thematrices. Thedrug release mechanisms were determined byfitting thedissolution data into classic kinetic equations. Results. Irvingia gabonensis polymer deformed plastically with afast onset and ahigh amount ofplastic deformation compared with xanthan gum and HPMC. This polymer was directly compressible and formed intact non-disintegrating tablets; themechanical and dissolution properties ofIrvingia gabonensis polymer tablets generally decreased with increasing concentration ofibuprofen. Theranking ofdissolution times was xanthan gum> freeze-dried Irvingia gabonensis> HPMC> oven-dried Irvingia gabonensis. Theaddition oftheexcipients improved themechanical properties ofthetablets, aided ibuprofen release, and altered therelease kinetics, which was largely defined bytheKorsmeyer–Peppas model. Increasing theproportion ofxanthan gum and HPMC inthematrices resulted inadecreased amount ofibuprofen released after 9h, with xanthan gum having agreater effect. Conclusions. Irvingia gabonensis polymer matrices may be effective inthepreparation ofcontrolled release tablets, and their right combination with xanthan gum orHPMC could provide atime-independent release for longer durations.
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    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.
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    Material and compressional properties of Irvingia gabonensis (O’Rorke) Bail polymers
    (International Pharmaceutical Excipients Council (IPEC), 2022) Patani, B. O.; Akin-Ajani, O. D.; Kumaran, A.; Odeku, O. A
    The physicochemical, material and compressional properties of the Irvingia gabonensis (O’Rorke) Bail polymer were evaluated and compared with xanthan gum and hydroxypropylmethylcellulose (HPMC). The Irvingia polymer was extracted using established methods and processed using two methods of drying, that is, oven-drying and freeze-drying. The compression mechanisms were evaluated using the Heckel and Kawakita equations. The mechanical strength of the tablets was evaluated using crushing strength and friability. The results showed that the Irvingia kernel polymer was slightly acidic, free of heavy metals, with irregularly shaped particles that exhibited some degree of crystallinity. The Irvingia kernel polymer was directly compressible and formed intact non-disintegrating tablets similar to the standard polymers. The Heckel and Kawakita equations indicated that the Irvingia polymer deformed plastically with fast onset and a high amount of plastic deformation compared to xanthan gum and HPMC. The freeze-dried Irvingia gum showed significantly (p<0.05) higher crushing strength and lower friability than the oven-dried polymer. The results indicated that the drying method had a significant impact on the compression characteristics as well as the properties of the polymer tablets. Thus, the Irvingia polymer could be more suitable for the formulation of tablets using direct compression.
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    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.
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    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.
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    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.
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    Formulation of Diclofenac Sodium Emulsion Using Colocynthis Citrullus L. (Melon) Seed Oil
    (West African Postgraduate College of Pharmacists (WAPCP), 2019) Akin-Ajani, O. D.; Ajala T. O.; Ogunnubi M. A
    Background: Melon seed obtained from the fruit of Colocynthis citrullus L. is widely used in Nigeria as a soup thickener. The seed has a high oil yield (42-57%) which has been largely unexplored as excipient in pharmaceutical formulations. Objectives: To evaluate melon seed oil as a drug carrier in emulsion using diclofenac as a model drug. Methods: Melon seed oil was extracted and the physicochemical properties were characterised. The emulsions were prepared using the traditional wet and dry gum methods, and all the emulsions were evaluated using viscosity measurements, creaming rate, and in-vitro drug release. Results: Melon seed oil had a pale yellow colour, with characteristic taste, and a neutral pH. Melon seed oil exhibited higher acid, saponification and ester values than castor oil but lower iodine value indicating an edible non-drying oil, unsusceptible to auto-oxidation. Both oils achieved a great degree of emulsification with globule size < 15mm μm. Emulsions of melon seed oil were generally less viscous with a higher degree of creaming compared to castor oil emulsions. Diclofenac emulsions prepared with melon seed oil, however, were more viscous and gave the highest release of diclofenac irrespective of the method of preparation. Only diclofenac emulsion prepared with melon seed oil using the wet gum method had > 70 % release within 45 minutes thus meeting the official specification. Conclusion: Melon seed oil functioned as a drug carrier for diclofenac. Thus, it will find application in pharmaceutical emulsions.
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    Formulation and Antimicrobial Evaluation of Isopropyl Hand Sanitizer using Co-processed Excipients
    (African Journals OnLine, 2020-02) Akin-Ajani, O. D.; Ajala T. O.; Ogunnubi M. A
    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.