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  1. Evaluation of the stability of Yamakagashi (Rhabdophis tigrinus) Equine Antivenom after 20 years storage
    Morokuma K, Matsumura T, Yamamoto A, Sakai A, Hifumi T, Ato M, et al.
    Trop Biomed, 2021 Jun 01;38(2):111-118.
    PMID: 34172698 DOI: 10.47665/tb.38.2.042
    In 2000, an equine Yamakagashi (Rhabdophis tigrinus) antivenom (Lot 0001) was testmanufactured as an unapproved drug for treatment of Yamakagashi bites. It was stocked on the premise of super-legal use from the viewpoint of emergency health crisis management. The antivenom showed a strong neutralizing ability against the hemorrhagic and coagulation activity of the Yamakagashi venom in its potency test. One vial of the antivenom can effectively neutralize at least about 4 mg of Yamakagashi venom. Its efficacy has also been confirmed in patients with severe cases of R. tigrinus bite that has been used in emergency. In 2020, this antivenom (Lot 0001) has reached 20 years after its production. To evaluate the integrity and potency of the antivenom, quality control, safety and potency tests had been conducted almost every year since 2012. Physical and chemical tests (property test, moisture content test, insoluble foreign matter test, osmotic pressure ratio test, pH test, protein content test, endotoxin test, sterility test) of the antivenom, showed no significant changes throughout the years, when compared to the results immediately after its production in 2000. All the parameters measured were also within the standard values. In animal safety tests (test for absence of toxicity and pyrogen), there was no change in the test results during the storage period and no abnormalities were observed. The potency test (anti-coagulant activity) after 20 years of the product, showed the same potency as those recorded immediately after production. Therefore, in all of the stability monitoring tests conducted so far, the product did not show any significant change compared to the results immediately after production. This confirms the stability of the product during the stockpiling period to the present, that is, 20 years after production.
    Matched MeSH terms: Drug Stability*
  2. Current regulatory requirements and practical approaches for stability analysis of pharmaceutical products: A comprehensive review
    Sengupta P, Chatterjee B, Tekade RK
    Int J Pharm, 2018 May 30;543(1-2):328-344.
    PMID: 29635054 DOI: 10.1016/j.ijpharm.2018.04.007
    Different regulatory guidelines recommend establishing stability profile of pharmaceuticals at the time of drug development. The expiry date, retesting period and storage conditions of active drugs or products are established through stability analysis. Several regulatory guidelines exist for stability testing of pharmaceuticals. Mostly, ICH stability guidelines are followed in practice. This guideline recommends to validate stability indicating method using forced degradation samples that contains all possible degradation impurities. ICH guidelines provide general recommendations for inclusion of stability indicating parameters in a stability testing protocol. However, those guidelines do not provide specific requirements and experimental methodology to be followed for stability studies. Due to this gap, often confusion arises in the scientific community in designing stability testing protocol. Therefore, significant variations are observed in reported literature in selection of stability indicating parameters. Procedural dissimilarity amongst reported stability studies is also evident. This review discusses the regulatory guidelines and procedures to follow in performing stability testing of pharmaceuticals. Scope of this review also includes recommendations on practical approaches for designing stability testing protocol to fulfill current regulatory requirements for drug substances and their formulations.
    Matched MeSH terms: Drug Stability*
  3. Synthesis, characterization and physicochemical properties of oleic acid ether derivatives as biolubricant basestocks
    Salimon J, Salih N, Yousif E
    J Oleo Sci, 2011;60(12):613-8.
    PMID: 22123242
    Petroleum is a finite source as well as causing several environmental problems. Therefore petroleum needs to be replaced by alternative and sustainable sources. Plant oils and oleochemicals derived from them represent such alternative sources; the use of oleochemicals as biobased lubricants is of significant interest. This article presents a series of chemical modification on oleic acid to yield synthetic biolubricant basestocks. Measuring of density, volatility, cloud point (CP), pour point (PP), flash point (FP), viscosity index (VI), onset temperature (OT) and signal maximum temperature (SMT) was carried out for each compound. Furthermore, the friction and wear properties were measured using high-frequency reciprocating rig (HFRR). The results showed that octadecyl 9-octadecyloxy-10-hydroxyoctadecanoate exhibited the most favorable low-temperature performance (CP %ndash;26°C, PP %ndash;28°C) and the lowest ball wear scan diameter (42 µm) while propyl 9-propyloxy-10-hydroxyoctadecanoate exhibited the higher oxidation stability (OT 156°C).
    Matched MeSH terms: Drug Stability
  4. Fulltext Evaluation of cold chain monitoring in Kelantan, Malaysia
    Hanjeet K, Lye MS, Sinniah M, Schnur A
    Bull World Health Organ, 1996;74(4):391-7.
    PMID: 8823961
    An analysis was carried out on a total of 883 cold chain monitor (CCM) cards, which had been attached to batches of poliomyelitis, measles, DPT (diphtheria, pertussis, tetanus) and hepatitis B vaccines, during their transport and storage from the central store in Kuala Lumpur to Kelantan, a state in north-eastern Malaysia; 234 freeze watches attached to hepatitis B vaccines were also analysed. The monitor cards and freeze watches were observed at six levels between the central store and the periphery during distribution of the vaccines, and a colour change in any of the four windows (A, B, C, D) on the CCM cards or the freeze watches was recorded. In addition, 33 unopened vials of oral poliovirus vaccine (OPV), collected from refrigerators in 29 health facilities in Kelantan, were tested for potency using the tissue culture infective dose 50 (TCID50) method; 14 of them (42%) did not meet the WHO criteria for potent vaccines. The results showed that at the final destination 13.4% of all cards remained white while a colour change to blue was observed in 65% in window A, 16.6% in window B, and 4.4% in window C; none had turned blue in window D indicating that the vaccine had not been subjected to temperatures > or = 34 degrees C for 2 hours. All but 2 of the 234 freeze watches had turned purple, which indicates exposure of the hepatitis B vaccines to temperatures below 0 degree C. These results will assist health planners to correct the weaknesses identified in the cold chain system.
    Matched MeSH terms: Drug Stability*
  5. Understanding the Roles of Excipients in Moisture Management in Solid Dosage Forms
    Veronica N, Heng PWS, Liew CV
    Mol Pharm, 2024 May 06;21(5):2484-2500.
    PMID: 38647432 DOI: 10.1021/acs.molpharmaceut.4c00031
    Excipients are ubiquitous in pharmaceutical products, and often, they can also play a critical role in maintaining product quality. For a product containing a moisture-sensitive drug, moisture can be deleterious to the product stability during storage. Therefore, using excipients that interact with moisture in situ can potentially alleviate product stability issues. In this study, the interactive behavior of starch with moisture was augmented by coprocessing maize starch with sodium chloride (NaCl) or magnesium nitrate hexahydrate [Mg(NO3)2·6H2O] at different concentrations (5 and 10%, w/w). The effect of the formulation on drug stability was assessed through the degradation of acetylsalicylic acid, which was used as the model drug. The results showed that coprocessing of the starch with either NaCl or Mg(NO3)2·6H2O impacted the number of water molecule binding sites on the starch and how the sorbed moisture was distributed. The coprocessed excipients also resulted in lower drug degradation and lesser changes in tablet tensile strength during post-compaction storage. However, corresponding tablet formulations containing physical mixtures of starch and salts did not yield promising outcomes. This study demonstrated the advantageous concomitant use of common excipients by coprocessing to synergistically mitigate the adverse effects of moisture and promote product stability when formulating a moisture-sensitive drug. In addition, the findings could help to improve the understanding of moisture-excipient interactions and allow for the judicious choice of excipients when designing formulations containing moisture-sensitive drugs.
    Matched MeSH terms: Drug Stability*
  6. Fulltext Saponin Stabilization via Progressive Freeze Concentration and Sterilization Treatment
    Osman WNAW, Selvarajah D, Samsuri S
    Molecules, 2021 Aug 11;26(16).
    PMID: 34443445 DOI: 10.3390/molecules26164856
    Saponin is a biopesticide used to suppress the growth of the golden apple snail population. This study aims to determine the stabilized conditions for saponin storage. The maceration process was used for saponin extraction, and for saponin concentration, progressive freeze concentration (PFC) was used. Afterwards, stability analysis was performed by storing the sample for 21 days in two conditions: Room temperature (26 °C) and cold room (10 °C). The samples kept in a cold room were sterilized samples that undergo thermal treatment by placing the sample in the water bath. The non-sterilized samples were kept in room temperature condition for 21 days. The results showed that saponin stored in the cold room (sterilized sample) has low degradation with higher concentration than those stored at room temperature in stability analysis with the highest saponin concentration (0.730 mg/mL) at a concentration temperature of -6 °C and concentration time of 15 min. The lowest saponin concentration obtained by saponin stored at room temperature (non-sterilized sample) is 0.025 mg/mL at a concentration temperature of -6 °C and concentration time of 10 min. Thus, the finding concluded that saponin is sensitive to temperature. Hence, the best storage condition to store saponin after thermal treatment is to keep it in a cold room at 10 °C.
    Matched MeSH terms: Drug Stability
  7. Fulltext Preparation of astaxanthin nanodispersions using gelatin-based stabilizer systems
    Anarjan N, Nehdi IA, Sbihi HM, Al-Resayes SI, Malmiri HJ, Tan CP
    Molecules, 2014 Sep 10;19(9):14257-65.
    PMID: 25211006 DOI: 10.3390/molecules190914257
    The incorporation of lipophilic nutrients, such as astaxanthin (a fat soluble carotenoid) in nanodispersion systems can either increase the water solubility, stability and bioavailability or widen their applications in aqueous food and pharmaceutical formulations. In this research, gelatin and its combinations with sucrose oleate as a small molecular emulsifier, sodium caseinate (SC) as a protein and gum Arabic as a polysaccharide were used as stabilizer systems in the formation of astaxanthin nanodispersions via an emulsification-evaporation process. The results indicated that the addition of SC to gelatin in the stabilizer system could increase the chemical stability of astaxanthin nanodispersions significantly, while using a mixture of gelatin and sucrose oleate as a stabilizer led to production of nanodispersions with the smallest particle size (121.4±8.6 nm). It was also shown that a combination of gelatin and gum Arabic could produce optimal astaxanthin nanodispersions in terms of physical stability (minimum polydispersity index (PDI) and maximum zeta-potential). This study demonstrated that the mixture of surface active compounds showed higher emulsifying and stabilizing functionality compared to using them individually in the preparation of astaxanthin nanodispersions.
    Matched MeSH terms: Drug Stability
  8. Fulltext Physico-chemical properties of spray-dried red pitaya (Hylocereus polyrhizus) peel powder during storage
    Ee, S.C., Bakar, J., Kharidah, M., Dzulkifly, M.H., Noranizan, A.
    International Food Research Journal, 2014;21(3):1213-1218.
    MyJurnal
    The physico-chemical properties of spray-dried pitaya peel powders kept at accelerated (45 ± 2°C) and room temperature (28 ± 2°C) for 14 weeks and 6 months, respectively were evaluated. Changes in physico-chemical properties of the peel powder were used as indicators of stability, while changes of the betacyanin pigment retention was used to calculate the shelf-life of the powder. Storage temperatures significantly (p < 0.05) affected all the studied parameters and Hunter a value had the most significant change. The pigment retention of peel powder was approximately 87% at 45°C and 89% at room temperature storage. Degradation of betacyanin pigment in the powder followed the first order reaction kinetics with the half-life (t1/2) of approximately 76 weeks at 45°C and 38 months at 28°C. The spray-dried pitaya peel powder had a solubility of 87 to 92% and low in powder hygroscopicity. The final Aw of the powder did not exceed 0.6 for both storage temperatures.
    Matched MeSH terms: Drug Stability
  9. Relative Humidity Cycling: Implications on the Stability of Moisture-Sensitive Drugs in Solid Pharmaceutical Products
    Veronica N, Heng PWS, Liew CV
    Mol Pharm, 2023 Feb 06;20(2):1072-1085.
    PMID: 36480246 DOI: 10.1021/acs.molpharmaceut.2c00812
    The stability of a moisture-sensitive drug in tablet formulations depends particularly on the environment's relative humidity (RH) and the products' prior exposure to moisture. This study was designed to understand drug stability in relation to the moisture interaction of the excipients, moisture history of the tablets, and RH of the environment. The stability study was performed on tablets containing acetylsalicylic acid (ASA), formulated with common pharmaceutical excipients like native maize starch, microcrystalline cellulose (MCC), partially pregelatinized maize starch (PGS), dicalcium phosphate dihydrate (DCP), lactose, and mannitol. The tablets were subjected to storage conditions with RH cycling alternating between 53% and 75%. Results were also compared to tablets stored at a constant RH of 53% or 75%. The excipients demonstrated marked differences in their interactions with moisture. They could be broadly grouped as excipients with RH-dependent moisture content (native maize starch, MCC, and PGS) and RH-independent moisture content (DCP, lactose, and mannitol). As each excipient interacted differently with moisture, degradation of ASA in the tablets depended on the excipients' ability to modulate the moisture availability for degradation. The lowest ASA degradation was observed in tablets formulated with low moisture content water-soluble excipients, such as lactose and mannitol. The impact of RH cycling on ASA stability was apparent in tablets containing native maize starch, MCC, PGS, or DCP. These findings suggested that the choice of excipients influences the effect of moisture history on drug stability. The results from studies investigating moisture interaction of excipients and drug stability are valuable to understanding the inter-relationship between excipients, moisture history, and drug stability.
    Matched MeSH terms: Drug Stability
  10. Evaluating the physicochemical properties and efficacy of recently expired and aged antivenom products from Thailand and Taiwan
    Tan KY, Liew ST, Tan QY, Abdul-Rahman FN, Azmi NI, Sim SM, et al.
    Toxicon, 2019 Mar 15;160:55-58.
    PMID: 30797900 DOI: 10.1016/j.toxicon.2019.02.010
    Gel filtration chromatography and gel electrophoresis revealed minimal protein degradation in lyophilized antivenoms which were 2-year expired (Hemato Polyvalent, Neuro Polyvalent; Thailand) and 18-year expired (Hemato Bivalent, Neuro Bivalent; Taiwan). All expired antivenoms retained immunological binding activity, and were able to neutralize the hemotoxic or neurotoxic as well as lethal effects of the homologous snake venoms. The findings show that antivenoms under proper storage conditions may remain relatively stable beyond the indicated shelf life.
    Matched MeSH terms: Drug Stability*
  11. Stability indicating HPLC-UV method for detection of curcumin in Curcuma longa extract and emulsion formulation
    Syed HK, Liew KB, Loh GO, Peh KK
    Food Chem, 2015 Mar 1;170:321-6.
    PMID: 25306352 DOI: 10.1016/j.foodchem.2014.08.066
    A stability-indicating HPLC-UV method for the determination of curcumin in Curcuma longa extract and emulsion was developed. The system suitability parameters, theoretical plates (N), tailing factor (T), capacity factor (K'), height equivalent of a theoretical plate (H) and resolution (Rs) were calculated. Stress degradation studies (acid, base, oxidation, heat and UV light) of curcumin were performed in emulsion. It was found that N>6500, T<1.1, K' was 2.68-3.75, HETP about 37 and Rs was 1.8. The method was linear from 2 to 200 μg/mL with a correlation coefficient of 0.9998. The intra-day precision and accuracy for curcumin were ⩽0.87% and ⩽2.0%, while the inter-day precision and accuracy values were ⩽2.1% and ⩽-1.92. Curcumin degraded in emulsion under acid, alkali and UV light. In conclusion, the stability-indicating method could be employed to determine curcumin in bulk and emulsions.
    Matched MeSH terms: Drug Stability
  12. Comparative study of the oxidative and physical stability of liposomal and nanoliposomal polyunsaturated fatty acids prepared with conventional and Mozafari methods
    Rasti B, Jinap S, Mozafari MR, Yazid AM
    Food Chem, 2012 Dec 15;135(4):2761-70.
    PMID: 22980870 DOI: 10.1016/j.foodchem.2012.07.016
    The relative oxidative stability of freshly prepared and stored liposomal and nanoliposomal systems of docosahexaenoic acid (DHA, 22:6 n-3) and eicosapentaenoic acid (EPA, 20:5 n-3) were investigated. The effects of organic solvents on the oxidative stability of liposomal polyunsaturated fatty acids (PUFAs) produced by two methods, the Bangham thin-film hydration (conventional rotary evaporation method and using organic solvents) and Mozafari (direct hydration and without using organic solvents) methods, were compared. The highest physicochemical stability was observed in PUFA liposomes prepared by the Mozafari method, followed by conventional liposomes and bulk PUFAs. There was no significant change in physicochemical stability during 10 months of cold storage (4°C) in the dark. Moreover, the comparison between liposomes (>200 nm) and nanoliposomes (50-200 nm) revealed that the surface charge, physical stability and oxidative stability of liposomal PUFAs increased as the size of the liposomes decreased. The differences in the oxidative stability of PUFAs may be due to the protective effects of aqueous systems, which indicate the advantage of using non-organic solvent (water and CO(2)) techniques in liposome manufacturing.
    Matched MeSH terms: Drug Stability
  13. Fulltext Boronate derivatives of functionally diverse catechols: stability studies
    Ketuly KA, Hadi AH
    Molecules, 2010 Apr;15(4):2347-56.
    PMID: 20428047 DOI: 10.3390/molecules15042347
    Benzeneboronate of catecholic carboxyl methyl esters, N-acetyldopamine, coumarin and catechol estrogens were prepared as crystalline derivatives in high yield. Related catechol compounds with extra polar functional group(s) (OH, NH2) do not form or only partially form unstable cyclic boronate derivatives.
    Matched MeSH terms: Drug Stability
  14. Role of blooming in determining the storage stability of lipid-based dosage forms
    Khan N, Craig DQ
    J Pharm Sci, 2004 Dec;93(12):2962-71.
    PMID: 15459945
    Gelucire 50/13 alone and solid dispersions in this material containing two model drugs (10% w/w caffeine and paracetamol) have been studied with a view to establishing the mechanism underpinning changes in drug-release characteristics as a function of storage time and temperature. The lipid systems were fabricated into tablets and stored for up to 180 days at temperatures of 20 and 37 degrees C. The dispersions were studied using differential scanning calorimetry (DSC), scanning electron microscopy, and dissolution testing. DSC studies indicated that the Gelucire 50/13 exists in two principal melting forms (melting points 38 and 43 degrees C) that undergo transformation to the higher melting form on storage at 37 degrees C. Scanning electron microscopy studies indicated that the systems exhibit "blooming," with crystal formation on the surface being apparent on storage at both temperatures. The dissolution rate increased on storage, with the effect being particularly marked at higher storage temperatures and for the paracetamol systems. However, whereas these changes corresponded well to those seen for the morphology, the correlation between the changes in dissolution and those of the DSC profiles was poor. The study has suggested a novel explanation for the storage instability of Gelucire 50/13 whereby the change in dissolution is associated not with molecular rearrangement as such but with the gross distribution of the constituent components, this in turn altering the physical integrity of the lipid bases.
    Matched MeSH terms: Drug Stability
  15. Cycloproprene fatty acids in Gnetum gnemon (L.) seeds and leaves
    Berry SK
    J Sci Food Agric, 1980 Jul;31(7):657-62.
    PMID: 6779057
    Matched MeSH terms: Drug Stability
  16. Ergometrine stability in postpartum haemorrhage kits: Does temperature and light matter?
    Donnan F, Senarathna SMDKG, Ware B, Rawlins MDM, Dontham C, Chuang VTG, et al.
    Aust N Z J Obstet Gynaecol, 2020 06;60(3):344-349.
    PMID: 31512230 DOI: 10.1111/ajo.13046
    BACKGROUND: Postpartum haemorrhage (PPH) kits containing uterotonics are used on obstetric units for the timely management of PPH. Visible discolouration of ergometrine and ergometrine-oxytocin injections was observed in PPH kits stored in medical refrigerators on the obstetric unit at our hospital.

    AIM: To investigate the stability of ergometrine and ergometrine-oxytocin injections in PPH kits under simulated clinical storage conditions and to determine the potency of ampoules quarantined from PPH kits on our obstetric unit.

    MATERIAL AND METHODS: Ergometrine and ergometrine-oxytocin injection ampoules were stored exposed to and protected from light at 4°C and room temperature (25°C) for up to three months, and assayed by high-performance liquid chromatography. Stability was based on the time for the ergometrine or oxytocin concentration to fall to 90% of the original concentration (t90 ). The potency of quarantined discoloured ampoules also was determined.

    RESULTS: Ergometrine was stable at both temperatures for >6 months, when stored protected from light in simulated clinical conditions. When exposed to light, ergometrine was stable for approximately 4 days at 25°C and 10 days at 4°C. Discoloured ergometrine and ergometrine-oxytocin injection ampoules were found to be <90% of the nominal concentration.

    CONCLUSION: Stability of ergometrine in PPH kits is largely unaffected by temperature fluctuations (at 4°C and 25°C) over 6 months when protected from light. Ergometrine and ergometrine-oxytocin ampoules should be inspected prior to use and any discoloured ampoules discarded.

    Matched MeSH terms: Drug Stability
  17. Exploring role of polysaccharides present in Ganoderma lucidium extract powder and probiotics as solid carriers in development of liquisolid formulation loaded with quercetin: A novel study
    Khursheed R, Singh SK, Gulati M, Wadhwa S, Kapoor B, Pandey NK, et al.
    Int J Biol Macromol, 2021 Jul 31;183:1630-1639.
    PMID: 34015408 DOI: 10.1016/j.ijbiomac.2021.05.064
    Ganoderma lucidium extract powder (GLEP) contains various polysaccharides which are well known for their antioxidant and anti-inflammatory actions. Probiotics (PB) are well-established for providing a plethora of health benefits. Hence, use of mushroom polysaccharides and probiotics as carriers to solidify liquisolid formulation is anticipated to function as functional excipients i.e. as adsorbent that may provide therapeutic benefits. Quercetin (QUR) has been used as model lipophilic drug in this study. QUR loaded liquisolid compacts (LSCs) were formulated using Tween 80 as solvent. These were further solidified using a combination of PB and GLEP as carriers. Aerosil-200 (A-200) was used as coating agent. The formulation exhibited very good flow characteristics. Dissolution rate of raw QUR was found to be less than 10% in 60 min while in case of QUR loaded LSCs, more than 90% drug release was observed within 5 min. Absence of crystalline peaks of QUR in the DSC and PXRD reports of LSCs and their porous appearance in SEM micrographs indicate that QUR was successfully incorporated in the LSCs. The developed formulation was found to be stable on storage under accelerated stability conditions.
    Matched MeSH terms: Drug Stability
  18. Chloride reduction by water washing of crude palm oil to assist in 3-monochloropropane-1, 2 diol ester (3-MCPDE) mitigation
    Lakshmanan S, Yung YL
    Food Addit Contam Part A Chem Anal Control Expo Risk Assess, 2021 Mar;38(3):371-387.
    PMID: 33596165 DOI: 10.1080/19440049.2020.1842516
    Chloride reduction in crude palm oil (CPO) of greater than 80% was achieved with water washing conducted at 90°C. Inorganic chloride content in CPO was largely removed through washing, with no significant reduction in the organic chloride. Phosphorous content of CPO reduced by 20%, while trace elements such as calcium, magnesium and iron were also reduced in the washing operation. The 3-MCPDE formed in the refined, bleached and deodorised palm oil displayed (RBDPO) a linear relationship with the chloride level in washed CPO, which could be represented by the equation y = 0.91x, where y is 3-MCPDE and x represents the chloride in RBDPO refined from washed CPO. In plant scale trials using 5% water at 90°C, mild acidification of the wash water at 0.05% reduced chloride by average 76% in washed CPO. Utilising selected bleaching earths, controlled wash water temperature and wash water volume produced low chloride levels in RBDPO. Chloride content less than 1.4 mg kg-1 in plant RBDPO production was achieved, through physical refining of washed CPO containing less than 2 mg kg-1 chloride and would correspond to 3-MCPDE levels of 1.25 mg kg-1 in RBDPO. The 3-MCPDE reduced further to 1.1 mg kg-1 as the chloride level of washed CPO decreased below 1.8 mg kg-1. Chloride has been shown to facilitate the 3-MCPDE formation and its removal in lab scale washing study has yielded lower 3-MCPDE levels formed in RBDPO. In actual plant operations using washed CPO, 3-MCPDE levels below 1.25 mg kg-1 were achieved consistently in RBDPO.
    Matched MeSH terms: Drug Stability
  19. Polymeric nanoparticles for topical delivery of alpha and beta arbutin: preparation and characterization
    Ayumi NS, Sahudin S, Hussain Z, Hussain M, Samah NHA
    Drug Deliv Transl Res, 2019 04;9(2):482-496.
    PMID: 29569027 DOI: 10.1007/s13346-018-0508-6
    To investigate the use of chitosan nanoparticles (CS-TPP-NPs) as carriers for α- and β-arbutin. In this study, CS-TPP-NPs containing α- and β-arbutin were prepared via the ionic cross-linking of CS and TPP and characterized for particle size, zeta potential, and dispersity index. The entrapment efficiency and loading capacity of various β-arbutin concentrations (0.1, 0.2, 0.4, 0.5, and 0.6%) were also investigated. SEM, TEM FTIR, DSC and TGA analyses of the nanoparticles were performed to further characterize the nanoparticles. Finally, stability and release studies were undertaken to ascertain further the suitability of the nanoparticles as a carrier system for α- and β-arbutin. Data obtained clearly indicates the potential for use of CS-TPP-NPs as a carrier for the delivery of α- and β-arbutin. The size obtained for the alpha nanoparticles (α-arbutin CSNPs) ranges from 147 to 274 d.nm, with an increase in size with increasing alpha arbutin concentration. β-arbutin nanoparticles (β-arbutin CSNPs) size range was from 211.1 to 284 dn.m. PdI for all nanoparticles remained between 0.2-0.3 while the zeta potential was between 41.6-52.1 mV. The optimum encapsulation efficiency and loading capacity for 0.4% α-arbutin CSNPs were 71 and 77%, respectively. As for β-arbutin, CSNP optimum encapsulation efficiency and loading capacity for 0.4% concentration were 68 and 74%, respectively. Scanning electron microscopy for α-arbutin CSNPs showed a more spherical shape compared to β-arbutin CSNPs where rod-shaped particles were observed. However, under transmission electron microscopy, the shapes of both α- and β-arbutin CSNP nanoparticles were spherical. The crystal phase identification of the studied samples was carried out using X-ray diffraction (XRD), and the XRD of both α and β-arbutin CSNPs showed to be more crystalline in comparison to their free form. FTIR spectra showed intense characteristic peaks of chitosan appearing at 3438.3 cm-1 (-OH stretching), 2912 cm-1 (-CH stretching), represented 1598.01 cm-1 (-NH2) for both nanoparticles. Stability studies conducted for 90 days revealed that both α- and β-arbutin CSNPs were stable in solution. Finally, release studies of both α- and β-arbutin CSNPs showed a significantly higher percentage release in comparison to α- and β-arbutin in their free form. Chitosan nanoparticles demonstrate considerable promise as a carrier system for α- and β-arbutin, the use of which is anticipated to improve delivery of arbutin through the skin, in order to improve its efficacy as a whitening agent.
    Matched MeSH terms: Drug Stability
  20. Prediction and elucidation of factors affecting solubilisation of imatinib mesylate in lipids
    Siram K, Divakar S, Raghavan CV, Marslin G, Rahman H, Franklin G
    Colloids Surf B Biointerfaces, 2019 Feb 01;174:443-450.
    PMID: 30497005 DOI: 10.1016/j.colsurfb.2018.11.033
    The physico-chemical properties of lipids influencing the solubilisation of imatinib mesylate (IM) in lipid matrix were evaluated and a statistical model to predict the same has been derived in the present study. After experimental quantification of IM solubility in various lipids, Hansen Hildebrand's total solubility parameters were calculated in order to study the role of various forces connected to lipid-drug interaction. To develop a relationship between the various descriptors of the lipids and experimental solubility of IM in lipids (% w/w), quantitative structure-solubility relationship (QSSR) was used. To generate equations that can predict the solubility of IM in lipids (%w/w), multiple linear regression was used. Amongst the various lipids tested, glyceryl monostearate and behenic acid solubilised the highest (6.19 ± 0.22%) and lowest (0.01 ± 0.01%) amounts of IM respectively. Our results suggested that alkyl chain length, polarity of the lipids, index of cohesive interaction in solids, estimated number of hydrogen bonds that would be accepted by the solute from water molecules in an aqueous solution, estimated number of hydrogen bonds that would be donated by the solute to water molecules in an aqueous solution and solvent accessible surface area collectively play a significant role in solubilising IM in the lipids. The equation developed could predict the solubility of IM in lipids with good accuracy (R2pred = 0.912).
    Matched MeSH terms: Drug Stability
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