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1.
Eur J Pharm Sci ; 159: 105727, 2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33484813

RESUMO

Aligned with efforts to overcome shortcomings of conventional oral dosage forms, mucoadhesive oral thin films have been the focus of drug development. Transmucosal drug delivery through oral cavity is a popular alternative to deliver many drugs due to several advantages over conventional oral delivery including greater bioavailability due to bypassing the first-pass effect and avoiding enzymatic or acid-related degradation in the gastrointestinal tract, faster onset of action, and better patient compliance particularly in geriatric and pediatric patients. Furthermore, among solid transmucosal delivery platforms, buccal and sublingual strips or patches are more attractive due to their flexibility, ease of administration, high patient compliance, and fast dissolution. They are also more stable compared to oral gels making them a desirable candidate to deliver many small and large molecules locally or systemically. Mucoadhesion and mechanical properties of oral films are crucial in their performance, and therefore ways to measure these properties are also similarly important. Since they are relatively new to the pharmaceutical market, there are currently no FDA-recommended or USP standard methods available to characterize such dosage forms. This review intends to cover and discuss various methods cited in the literature to measure and evaluate mucoadhesive and mechanical properties of oral films.

2.
Int J Pharm ; 577: 119037, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31953081

RESUMO

Spinal Cord Injury (SCI) is one of the leading causes of physical disability. In this study, spherical PLGA nanoparticles (NPs) containing ChABC enzyme were manufactured and fully characterized for SCI therapy. The NPs were used in the rat's contused spinal cord to assess the functional improvement and scar digestion. Twenty-three adult male Wistar rats (275 ± 25 g) were assigned into four groups of control, sham, blank-treated particle, and ChABC-treated particle. Throughout the survey, the BBB scores were obtained for all the groups. Finally, the injured sections of animals were dissected, and histological studies were conducted using Luxol fast blue and Bielschowsky. The biocompatibility and non-toxicity effects of the NPs on olfactory ensheathing cells (OECs) were confirmed by the MTT test. The flow-cytometry revealed the purity of cultured OECs with p75+/GFAP+ at around 87.9 ± 2.4%. Animals in the control and the blank-treated groups exhibited significantly lower BBB scores compared with the ChABC-treated particle group. Histological results confirmed the induced contusion models in the injured site. Myelin was observed in the treated groups, especially when the ChABC-loaded nanoparticles were utilized. The immunohistochemistry results indicated the scar glial degradation in animals treated by the ChABC-loaded particles. According to this study, the loaded particles can potentially serve as a suitable candidate for spinal cord repair, functional recovery and axonal regeneration.

3.
Int J Pharm ; 577: 119042, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31953084

RESUMO

Prescription opioids have widely been abused as an epidemic. In this research, we developed a drug composition based on the crosslinked carboxymethylcellulose (XCMC) and a drug model that can effectively deter abuse by injection via multiple mechanisms. The anionic nature of the XCMC is responsible for complexing the cationic opioids in aqueous solutions, minimizing the free drug amount accessible for extraction. The crosslinked nature of the polymer is responsible for its swelling and partial containment of the drug solution within the swollen polymer's network, thus minimizing the available volume for subsequent injection. We have shown that XCMC can efficiently interact with cationic drugs in the form of physical blends and chemical complexes in different aqueous solvents, forming abuse-deterrent complexes. The complexation efficiency was affected by the solution pH and ionic strength, as well as the drug to polymer ratio in the formulation. The in vitro dissolution studies were conducted in two stages, the stage I in 0.1 M HCl and the stage II in water and pH 7.5 phosphate buffer. These studies confirmed the proper drug release under the legitimate conditions of use. Therefore, the XCMC polymers have a great potential to be used as deterring agents in developing opioid medications with abuse-deterrent properties.


Assuntos
Formulações de Dissuasão de Abuso/métodos , Analgésicos Opioides/administração & dosagem , Carboximetilcelulose Sódica/química , Analgésicos Opioides/química , Química Farmacêutica , Liberação Controlada de Fármacos , Concentração de Íons de Hidrogênio , Transtornos Relacionados ao Uso de Opioides/prevenção & controle , Concentração Osmolar , Solventes/química , Abuso de Substâncias por Via Intravenosa/prevenção & controle
4.
Int J Pharm ; 569: 118602, 2019 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-31394182

RESUMO

An innovative abuse-deterrent composition was developed to deter the most dangerous route of drug abuse, the intravenous route. The composition is based on a crosslinked sodium starch glycolate (X-SSG) that can effectively complex with cationic drugs in aqueous solutions and minimize the amount of the free drug available for extraction. Furthermore, the crosslinked polymer swells in and entraps a portion of the drug solution by which it reduces the available volume for syringing and subsequent injection. Two deterrent compositions were prepared, a drug-polymer physical blend and a drug-polymer chemical complex. The composition in its complexed form showed greater deterrence capacity than the physical blend except in solvents with ionic moieties, where the deterrence remained almost the same. The studies revealed that the complexation with the drug played a major role in total drug entrapment. Tablets prepared from the drug-polymer complex showed a complete and immediate drug release in 0.1 N HCl within the first 15 min. Moreover, the dissolution studies in the simulated intestinal media ruled out the re-complexation potential between the drug and the polymer. The proposed X-SSG composition provides a desirable drug release in the gastric and intestinal media under the legitimate use while deterring an intravenous abuse.


Assuntos
Formulações de Dissuasão de Abuso , Amido/análogos & derivados , Liberação Controlada de Fármacos , Suco Gástrico/química , Secreções Intestinais/química , Amido/química , Comprimidos
5.
Adv Pharm Bull ; 9(2): 241-248, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31380249

RESUMO

Purpose: We aimed to evaluate the effect of blueberry extract and microparticles (MP) on sunscreen performance of multifunctional cosmetics. Octocrylene (OCT), benzophenone-3 (BENZ-3) and Tinosorb® M (MBBT) were employed as UV filters. Methods: An in-silico modeling was used to determine the UV filters concentrations to obtain high values of sunscreen protection factor (SPF) and UVA protection factor (UVA-PF). MBBT and blueberry-loaded microparticles (MPMB+B) and MBBT-loaded microparticles (MPMBBT) were prepared by spray-drying. OCT and BENZ-3 were added in the oil phase of cosmetics. Cosmetics A and B contained MPMB+B and MPMBBT, respectively, and cosmetic C was prepared without MP. Characterization, physicochemical stability and in vitro SPF was performed. UV filters distribution in human stratum corneum (SC) for each cosmetic was performed. Anti-oxidant activity of blueberry extract was evaluated. Results: Sunscreen combination with the highest SPF was selected for formulations. Formulations A and B maintained their rheological behavior over time, unlike formulation C. In-vitro SPFs for formulations A, B and C were 51.0, 33.7 and 49.6, respectively. We also developed and validated a method for analysis of the UV filters by HPLC/ PDA suitable for the in-vivo assay. In Tape stripping test, MBBT showed SC distribution similar for all cosmetic formulations. OCT and BENZ-3 distribution to formulation A and C was also similar. Blueberry extract showed antioxidant capacity of 16.71 µg/mL equivalent to vitamin C. Conclusion: Cosmetics containing MPs presented better physical stability. Blueberry increased the photoprotective capacity of the formulations and added extra benefits due to its anti-oxidant and anti-aging properties.

6.
Expert Opin Drug Metab Toxicol ; 14(12): 1255-1271, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30408424

RESUMO

INTRODUCTION: Prescription opioid abuse is now an epidemic that has forced the government and industries to take initiatives. These include developing abuse-deterrent formulations (ADFs), issuing regulatory guidances and allocating massive budgets to ensure the safety and effectiveness of these medications. Areas covered: This review covers the regulatory guidance on evaluation and labeling of the branded and generic ADFs. It also includes the relevant patents and technologies, the in-vitro, in-vivo, the post-marketing data, the FDA reviews, and the products' labeling of the FDA-approved products with abuse-deterrent features. Expert opinion: Despite the development of a dozen products with abuse-deterrent features, most of these technologies rely on the same deterrent agent, making it easier for abusers to focus their manipulation efforts and share their experience to defeat the technology. Further advancement in the field requires developing more robust, more diverse, safer, and affordable deterrent technologies for the extended- and immediate-release opioid products. Moreover, advances in the reporting of the post-market results, issuance of policies in support of the ADFs, and concurrent monitoring of the illicit opioid market are other considerations that can further help in confronting the epidemic.


Assuntos
Formulações de Dissuasão de Abuso , Analgésicos Opioides/administração & dosagem , Transtornos Relacionados ao Uso de Opioides/prevenção & controle , Analgésicos Opioides/efeitos adversos , Desenho de Fármacos , Rotulagem de Medicamentos , Humanos , Transtornos Relacionados ao Uso de Substâncias/prevenção & controle , Estados Unidos , United States Food and Drug Administration
7.
Adv Pharm Bull ; 8(3): 495-505, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30276147

RESUMO

Purpose: The purpose of this study was to determine the effects of thermal processing and antioxidant formulation variables on the abuse deterrence performance of a high molecular weight poly(ethylene oxide) (PEO) polymer. Methods: A 24 factorial design with one categorical factor (antioxidant type) and three continuous factors (curing time, curing temperature, % antioxidant) was used. Abuse deterrence performance was evaluated using solution viscosity, surface melting temperature, and mechanical strength. Thermal degradation of PEO powders before compaction was also studied using DSC, FTIR spectroscopy, and viscosity analysis. Results: Our results showed that curing temperature and type of antioxidant can significantly affect the deterrence performance of PEO. The main effect plot for viscosity shows the most prominent factors affecting viscosity are curing temperature and type of antioxidant. However, curvature in the linear model obtained was not sufficient to completely describe the behavior. For surface melting temperature, butylated hydroxytoluene was associated with higher surface melting temperatures compared to ascorbic acid. Additionally, higher percent of antioxidant resulted in higher melting temperature. Particle size distribution to indicate mechanical strength showed no significant effects of tested factors. This suggests that comminution method has more prominent effect on tablet fragment size than the formulation and processing factors studied. Conclusion: While heat confers the mechanical strength to the polymer, it can diminish its physical stability and solution state viscosity. The experimental studies showed that prolonged exposure to high temperatures, even in the presence of antioxidants, can severely hamper polymer deterrence performance in both solid and solution states.

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