scholarly journals NIOSOMES AS AN APPROACH TO IMPROVE THE SOLUBILITY AND BIOAVAILABILITY OF BCS CLASS II DRUGS

Author(s):  
GAURANG SAWANT ◽  
GEETA BHAGWAT

Based on their solubility and permeability, drugs are typically divided into four classes (Classes I–IV) according to the biopharmaceutics classification system (BCS). Of these classes, BCS class II drugs have high permeability and low solubility; not only do these characteristics constitute the rate-limiting step in the formulation of these drugs but the low solubility in water results in low bioavailability. Thus, methods for improving their solubility have been developed using lipid carriers such as liposomes, niosomes, and aquasomes; other approaches include self-micro-emulsifying drug delivery systems (SMEDDS) and self-nano-emulsifying drug delivery systems (SNEDDS). Currently, niosome-based drug delivery systems that utilize nonionic surfactants, drugs, and cholesterol in varying ratios are being widely used to deliver both hydrophilic and lipophilic drugs in addition to several other applications of niosomes.

2021 ◽  
Vol 14 (11) ◽  
pp. 1201
Author(s):  
Bharti Gupta ◽  
Varsha Mishra ◽  
Sankalp Gharat ◽  
Munira Momin ◽  
Abdelwahab Omri

One of the major impediments to drug development is low aqueous solubility and thus poor bioavailability, which leads to insufficient clinical utility. Around 70–80% of drugs in the discovery pipeline are suffering from poor aqueous solubility and poor bioavailability, which is a major challenge when one has to develop an ocular drug delivery system. The outer lipid layer, pre-corneal, dynamic, and static ocular barriers limit drug availability to the targeted ocular tissues. Biopharmaceutical Classification System (BCS) class II drugs with adequate permeability and limited or no aqueous solubility have been extensively studied for various polymer-based solubility enhancement approaches. The hydrophilic nature of cellulosic polymers and their tunable properties make them the polymers of choice in various solubility-enhancement techniques. This review focuses on various cellulose derivatives, specifically, their role, current status and novel modified cellulosic polymers for enhancing the bioavailability of BCS class II drugs in ocular drug delivery systems.


2020 ◽  
Vol 27 (8) ◽  
pp. 1308-1336 ◽  
Author(s):  
Inese Mierina ◽  
Reinis Vilskersts ◽  
Māris Turks

Birch-bark triterpenoids and their semi-synthetic derivatives possess a wide range of biological activities including cytotoxic effects on various tumor cell lines. However, due to the low solubility and bioavailability, their medicinal applications are rather limited. The use of various nanotechnology-based drug delivery systems is a rapidly developing approach to the solubilization of insufficiently bioavailable pharmaceuticals. Herein, the drug delivery systems deemed to be applicable for birch-bark triterpenoid structures are reviewed. The aforementioned disadvantages of birch-bark triterpenoids and their semi-synthetic derivatives can be overcome through their incorporation into organic nanoparticles, which include various dendrimeric systems, as well as embedding the active compounds into polymer matrices or complexation with carbohydrate nanoparticles without covalent bonding. Some of the known triterpenoid delivery systems consist of nanoparticles featuring inorganic cores covered with carbohydrates or other polymers. Methods for delivering the title compounds through encapsulation and emulsification into lipophilic media are also suitable. Besides, the birch-bark triterpenoids can form self-assembling systems with increased bio-availability. Even more, the self-assembling systems are used as carriers for delivering other chemotherapeutic agents. Another advantage besides increased bioavailability and anticancer activity is the reduced overall systemic toxicity in most of the cases, when triterpenoids are delivered with any of the carriers.


MedChemComm ◽  
2016 ◽  
Vol 7 (10) ◽  
pp. 1881-1897 ◽  
Author(s):  
Noorul Adawiyah ◽  
Muhammad Moniruzzaman ◽  
Siti Hawatulaila ◽  
Masahiro Goto

The pharmaceutical industries face a series of challenges in the delivery of many newly developed drug molecules because of their low solubility, bioavailability, stability and polymorphic conversion.


2019 ◽  
Vol 4 (3) ◽  
pp. 160-175 ◽  
Author(s):  
Salome A. Chime ◽  
Paul A. Akpa ◽  
Anthony A. Attama

Lipid based excipients have gained popularity recently in the formulation of drugs in order to improve their pharmacokinetic profiles. For drugs belonging to the Biopharmaceutics Classification System (BCS) class II and IV, lipid excipients play vital roles in improving their pharmacokinetics properties. Various nanocarriers viz: Solid lipid nanoparticles, nanostructured lipid carriers, selfnanoemulsifying drug delivery systems (SNEDDS), nanoliposomes and liquid crystal nanoparticles have been employed as delivery systems for such drugs with evident successes. Lipid-based nanotechnology have been used to control the release of drugs and have utility for drug targeting and hence, have been used for the delivery of various anticancer drugs and for colon targeting. Drugs encapsulated in lipids have enhanced stability due to the protection they enjoy in the lipid core of these nanoformulations. However, lipid excipients could be influenced by factors which could affect the physicochemical properties of lipid-based drug delivery systems (LBDDS). These factors include the liquid crystalline phase transition, lipid crystallization and polymorphism amongst others. However, some of the physicochemical properties of lipids made them useful as nanocarriers in the formulation of various nanoformulations. Lipids form vesicles of bilayer which have been used to deliver drugs and are often referred to as liposomes and nanoliposomes. This work aims at reviewing the different classes of lipid excipients used in formulating LBDDS and nanoformulations. Also, some factors that influence the properties of lipids, different polymorphic forms in lipid excipients that made them effective nanocarriers in nano-drug delivery would be discussed. Special considerations in selecting lipid excipients used in formulating various forms of nanoformulations would be discussed.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1052
Author(s):  
Reem Abou Assi ◽  
Ibrahim M. Abdulbaqi ◽  
Toh Seok Ming ◽  
Chan Siok Yee ◽  
Habibah A. Wahab ◽  
...  

Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.


2022 ◽  
pp. 259-276
Author(s):  
Ayodeji Ojo Oteyola ◽  
Raffaele Pilla ◽  
Folasade Adesola Ola-Oladimeji ◽  
Omotayo Fagbuaro

Prostate cancer (PCa) is a global issue with increasing rise in morbidity and mortality. PCa treatment has been a global challenge for many years because drugs designed to combat this disease might show low efficacy as a result of low solubility. Limitations of chemo-drugs for treating PCa give birth to the use of nanomedicine which helps to improve drug delivery systems. Nanoemulsions are particles that are pharmaceutically formulated and comprised within the range of a nanometer (10-200nm). Nanoemulsions are thermodynamically stable and made up of safe gradient agents. This chapter elucidates the physiological, biological, and molecular barriers affecting drug delivery in PCa. The authors discussed the importance of nanoemulsions as potential drug delivery mechanisms in PCa therapy. This chapter focuses on reviewing different ways by which nanoemulsion can bring solution to water-solubility problems and also target specific cancer cells. Limitations of nanoemulsions in the drug delivery field were also highlighted.


2021 ◽  
Vol 11 ◽  
Author(s):  
Braham Dutt ◽  
Manjusha Choudhary ◽  
Vikas Budhwar

Background: The low solubility of an active pharmaceutical ingredient particularly biopharmaceutics classification system (BCS) Class II drugs leads to lower dissolution profile which in result cause reduction in overall bioavailability of drugs. Numerous approaches like nanotechnology, solid dispersion technique, micronization techniques etc were aimed by scientists in the past to resolve this issue, but still not enough to get the desired outcomes. Objective: Key focus of this review is study of advantages and disadvantages of cocrystallization, nanotechnology and solid dispersions drug delivery techniques and benefits of using cocrystallization techniques over above-mentioned techniques. Methods: Various parameters including pharmaceutical, pharmacological and toxicological effects related to these mentioned drug delivery systems have been compared. There advantages and disadvantages have been elaborated. Result: For drug delivery purpose, cocrystallization process has numerous advantages over nanotechnology and solid dispersions drug delivery techniques discussed in the text. Cocrystallization is newer technique that can modify the physicochemical and pharmaceutical properties of active pharmaceutical ingredients (API) are having issues like low solubility, low stability or sensitivity toward environmental hazards like temperature, moisture or photostability issues. During cocrystallization, drug and coformer interact with each other non-covalently in a fixed stoichiometric ratio. The availability of large amount of coformers make this technique to be favourable for the researchers in designing cocrystals of newer and older API’s. Conclusion: Although, solid dispersions and nanotechnology techniques are being utilised to a larger extent but still there are some drawbacks of these techniques like stability, toxicological factors and protection from environmental factors needs to be considered, while cocrystallization process drastically modifies the various pharmaceutical parameters without altering the pharmacological properties of API’s. Here in this review we performed a comparative analysis between nanotechnology, solid dispersion and cocrystallization techniques along with importance of cocrystallization in modification of drug profile and various applications of it in pharmaceutical and allied industry.


Author(s):  
SILVIA SURINI ◽  
DIAN NOVITASARI ◽  
ARRY YANUAR

Objective: Lansoprazole (LPZ) is a Biopharmaceutics Classification System Class II drug. It has low solubility and high permeability, so its rate ofdissolution is a rate-limiting step for drug absorption. This study aimed to improve the dissolution rate of LPZ by forming cocrystals, using nicotinamide(NCT) as the conformer.Methods: Cocrystals of LPZ were produced using the solvent evaporation and solvent-drop grinding methods with a molar ratio of 1:1 and 1:2.The cocrystals were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), and differential scanningcalorimetry (DSC). The solubility and dissolution of the LPZ cocrystals were examined in distilled water.Results: FTIR was used to confirm the formation of hydrogen bonds between LPZ and NCT. DSC and XRD studies showed the formation of crystalsfrom cocrystals and a decrease of the melting point of the cocrystals. The dissolution study revealed that the cocrystals could increase the LPZdissolution rate by up to 8.4-fold compared with pure LPZ.Conclusion: LPZ cocrystal formation with NCT was successful in increasing the dissolution rate of LPZ.


2021 ◽  
Vol 9 ◽  
Author(s):  
Chen Li ◽  
Ke Wang ◽  
Dong Xie

Ibuprofen is a potent non-steroidal anti-inflammatory drug due to its analgesic, antipyretic, and anti-inflammatory actions. However, its poor solubility in water makes it difficult to manufacture ibuprofen tablets, which limited the application of ibuprofen in drug delivery systems. Polymer–drug aerogels have attracted huge interest in optimizing the drug delivery efficiency and improving the physicochemical characteristics and therapeutic quality. Here, chitosan–ibuprofen aerogels with excellent swelling, high biocompatibility, and better drug delivery efficiency were synthesized by a simple method. Our study found that the chitosan–ibuprofen aerogels exhibited remarkably improved thermal stability, excellent swelling ratio, and high drug loading. As a consequence of these favorable properties, the chitosan–ibuprofen aerogels exhibited improved drug delivery efficiency and achieved drug prolonged administration. Our study highlights the great potential of polymer–drug aerogels in improving the drug delivery efficiency of transdermal drug delivery systems.


Author(s):  
G.E. Visscher ◽  
R. L. Robison ◽  
G. J. Argentieri

The use of various bioerodable polymers as drug delivery systems has gained considerable interest in recent years. Among some of the shapes used as delivery systems are films, rods and microcapsules. The work presented here will deal with the techniques we have utilized for the analysis of the tissue reaction to and actual biodegradation of injectable microcapsules. This work has utilized light microscopic (LM), transmission (TEM) and scanning (SEM) electron microscopic techniques. The design of our studies has utilized methodology that would; 1. best characterize the actual degradation process without artifacts introduced by fixation procedures and 2. allow for reproducible results.In our studies, the gastrocnemius muscle of the rat was chosen as the injection site. Prior to the injection of microcapsules the skin above the sites was shaved and tattooed for later recognition and recovery. 1.0 cc syringes were loaded with the desired quantity of microcapsules and the vehicle (0.5% hydroxypropylmethycellulose) drawn up. The syringes were agitated to suspend the microcapsules in the injection vehicle.


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